Linker ID	LIN0EBJON
Linker Name	Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
Linker Type	Flexible dual-reactive (amino/thiol) linker
Antibody-Linker Relation	Uncleavable
Structure
	3D MOL			2D MOL
Formula	C16H18N2O6
Isosmiles	C1CC(CCC1CN2C(=O)C=CC2=O)C(=O)ON3C(=O)CCC3=O
PubChem CID	125175
InChI	InChI=1S/C16H18N2O6/c19-12-5-6-13(20)17(12)9-10-1-3-11(4-2-10)16(23)24-18-14(21)7-8-15(18)22/h5-6,10-11H,1-4,7-9H2
InChIKey	JJAHTWIKCUJRDK-UHFFFAOYSA-N
IUPAC Name	(2,5-dioxopyrrolidin-1-yl) 4-[(2,5-dioxopyrrol-1-yl)methyl]cyclohexane-1-carboxylate
Pharmaceutical Properties	Molecule Weight		334.32	Polar area		101
	Complexity		599	xlogp Value		-0.1
	Heavy Count		24	Rot Bonds		5
	Hbond acc		6	Hbond Donor		0

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Objective Response Rate (ORR)	21.40%	Positive HER2 expression (HER2 +++/++)
Patients Enrolled	Untreated, asymptomatic BM or controlled brain disease treated with radiotherapy >14 days before enrollment; had received prior HER2-targeted therapy and chemotherapy; and had progressed on or after their most recent treatment of advanced breast cancer.
Administration Dosage	3.6 mg/kg intravenously every 3 weeks.
Related Clinical Trial
NCT Number	NCT01702571	Clinical Status	Phase 3
Clinical Description	A two-cohort, open-label, multicenter study of trastuzumab emtansine (T-DM1) in HER2-positive locally advanced or metastatic breast cancer patients who have received prior anti-HER2 and chemotherapy-based treatment.
Primary Endpoint	Objective response rate=21.40% (95% CI 14.60-29.60), clinical benefit rate=42.90% (95% CI 34.10-52.00).
Other Endpoint	Median PFS=5.50 months (95% CI, 5.30-5.60), overall survival =18.90 months (95% CI, 17.10-21.30).
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Objective Response Rate (ORR)	5.10%	Positive HER2 expression (HER2+++/++)
Patients Enrolled	HER2 positive advanced urothelial bladder cancer or pancreatic cancer/cholangiocarcinoma
Administration Dosage	Received singleagent TDM1 2.4 mg/kg once weekly (qw) or 3.6 mg/kg every 3 weeks (q3w).
Related Clinical Trial
NCT Number	NCT02999672	Clinical Status	Phase 2
Clinical Description	A study to determine best tumor response with trastuzumab emtansine in human epidermal growth factor receptor 2 (HER2) overexpressing solid tumors (KAMELEON).
Primary Endpoint	BOR, Urothelial bladder cancer (n=13); PR N=5 (38.46%);SD N=1 (7.7%);PD N=6 (46.2%);NE N=1 (7.69%). Pancreatic cancer/cholangiocarcinoma (n=7) PR N=1 (14.29%);SD N=3 (42.86%);PD N=2 (28.57%); NE N=1 (14.29%).
Other Endpoint	PFS, Urothelial bladder cancer (n=13), Median PFS, months (95% CI) 2.20 (1.18-4.30), Median OS, months (95% CI) 7.03 (3.75-NE). Pancreatic cancer/cholangiocarcinoma (n=7), Median PFS, months (95% CI) 2.58 (1.31-9.99), Median OS, months (95% CI) NE (1.45-NE).
Experiment 3 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Objective Response Rate (ORR)	5.60% (Day 21)
Patients Enrolled	38 patients were enrolled and 36 included in efficacy analysis.Patients were treated with the standard intravenous dosing of T- DM1, that is 3.6mg/kg every 3 weeks for a 21-day cycle.
Administration Dosage	3.6 mg/kg every 3 weeks for a 21-day cycle, until toxicity or progression.
Related Clinical Trial
NCT Number	NCT02465060	Clinical Status	Phase 2
Clinical Description	Targeted therapy directed by genetic testing in treating patients with advanced refractory solid tumors, lymphomas, or multiple myeloma (the MATCH screening trial).
Primary Endpoint	ORR was 2/36 (5.56%) with 90% confidence interval (90% CI, 1.00% to 16.50%)
Other Endpoint	6-mouth sPFS=23.60%.
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Objective Response Rate (ORR)	45.00%	Positive HER2 expression (HER2 +++/++)
Patients Enrolled	An Eastern Cooperative Oncology Group performance status of 0 or 1 and centrally confirmed, measurable, HER2-positive advanced breast cancer previously treated with trastuzumab and a taxane.
Administration Dosage	3.6 mg/kg ( trastuzumab emtansine) and 1200 mg (Atezolizumab) intravenously every 3 weeks.
Related Clinical Trial
NCT Number	NCT02924883	Clinical Status	Phase 2
Clinical Description	A randomized, multicenter, double-blind, placebo-controlled phase II study of the efficacy and safety of trastuzumab emtansine in combination with atezolizumab or atezolizumab-placebo in patients with HER2-positive locally advanced or metastatic breast cancer who have received prior trastuzumab and taxane based therapy.
Primary Endpoint	Median PFS=8.20 months (95% CI 5.80-10.70).
Other Endpoint	Median overall survival was not estimable (95% CI NE-NE); Objective response rate=45.00% (95% CI 28.06-50.30).
Experiment 5 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Objective Response Rate (ORR)	20.00%	High HER2 expression (HER2+++)
Patients Enrolled	HER2-positive, metastatic breast cancer previously treated with taxane, trastuzumab, and pertuzumab, and were T-DM1-nave.
Administration Dosage	The study consisted of a dose de-escalation (dose-finding) cohort, followed by an expansion cohort at the recommended phase II dose (RP2D), T-DM1 3.60 mg/kg intravenously every 21 days, and pembrolizumab 200mg intravenously every 21 days, if one or fewer DLTs were noted in the first six patients at that dose level, it would be declared the RP2D.
Related Clinical Trial
NCT Number	NCT03032107	Clinical Status	Phase 1b
Clinical Description	A phase 1b study of pembrolizumab in combination with trastuzumab-dm1 in metastatic HER2-positive breast cancer.
Primary Endpoint	OrR=20.00% (95% CI 5.70%-43.70%), and median PFS=9.60 months (95%CI 2.80-16.00 months).
Other Endpoint	There were no dose-limiting toxicities. The RP2D was 3.60 mg/kg T-DM1 plus 200 mg pembrolizumab every 21 days.
Experiment 6 Reporting the Activity Date of This ADC					[6]
Patients Enrolled	Newly diagnosed, HER2-positive, nonmetastatic, histologically confirmed, operable primary invasive breast carcinoma.
Administration Dosage	T-DM1 was dosed at 3.60 mg/kg once every 3 weeks. Trastuzumab was dosed at 6 mg/kg once every 3 weeks after an 8 mg/kg loading dose and started concurrently with the taxane. Pertuzumab was dosed at 420 mg once every 3 weeks after an 840 mg loading dose and administered concurrently with T-DM1 or trastuzumab-plus-taxane. An interval of 3 weeks from the last dose of anthracycline to initiation of HER2-targeted therapy was required. After the taxane-concurrent phase in the trastuzumab-containing arm, trastuzumab-plus-pertuzumab was continued for 1 year. In the T-DM1containing arm, T-DM1-plus-pertuzumab was continued for 1 year.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01966471	Clinical Status	Phase 3
Clinical Description	A randomized, multicenter, open-label, phase 3 trial comparing trastuzumab plus pertuzumab plus a taxane following anthracyclines versus trastuzumab emtansine plus pertuzumab following anthracyclines as adjuvant therapy in patients with operable HER2-positive primary breast cancer.
Primary Endpoint	82 (9.90%) IDFS events had occurred in the AC-THP arm and 80 (9.60%) had occurred in the AC-KP arm.
Other Endpoint	3-year IDFS rates were 94.10% (95% CI, 92.50 to 95.70) with AC-THP and 92.80% (95% CI, 91.00 to 94.50) with AC-KP.

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.10% (Day 28)	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST565)
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.20% (Day 28)	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST313)
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.60% (Day 28)	High HER2 expression (HER2+++)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX model: NIBIO G016)
Experiment 4 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.20% (Day 21)	Moderate HER2 expression (HER2++)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST225)
Experiment 5 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.40%	Positive HER2 expression (HER2+++/++)
Method Description	T-DM1 (Genentech) was administered i.p. at 10 mg/kg once per week.
In Vivo Model	Breast cancer PDX model (PDX: PDX12)

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 7.10% (Day 21)	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; CFPAC-1 (low-expression). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	CFPAC-1 cell line xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	CFPAC-1 cells		CVCL_1119
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.50% (Day 7)	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 1 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.10% (Day 48)	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 0.3 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 4 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 31.70% (Day 21)	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; Capan-1 (weak positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Capan-1 cell line xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 5 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.10% (Day 21)	Negative HER2 expression (HER2-)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; GCIY (negative). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	GCIY cell line xenograft model
In Vitro Model	Gastric adenocarcinoma	GCIY cells		CVCL_1228
Experiment 6 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.00% (Day 33)	Moderate HER2 expression (HER2++)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	HT29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 7 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.00% (Day 33)	Low HER2 expression (HER2 +)
Method Description	SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.00% (Day 58)	Low HER2 expression (HER2 +)
Method Description	11-18 cells (4,000,000 ) and HCC827 cells (2,000,000 ) were injected subcutaneously into the backs on both sides of the mice. T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	11-18 CDX model
In Vitro Model	Lung adenocarcinoma	11-18 cells		CVCL_6659
Experiment 9 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.00% (Day 58)	Low HER2 expression (HER2+)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	11-18 CDX model
In Vitro Model	Lung adenocarcinoma	11-18 cells		CVCL_6659
Experiment 10 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.30% (Day 30)	Positive HER2 expression (HER2 +++/++)
Method Description	Trastuzumab-emtansine (3 mg/kg, every seven days 4) induces efficient tumor cell killing in cell line-derived models of BT-474/R1-7 cells with HER2 expression with high expression.
In Vivo Model	BT-474 CDX model (T-DM1 resistant)
In Vitro Model	Invasive breast carcinoma	BT-474 cells (Trastuzumab emtansine resistant)		CVCL_0179
Experiment 11 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.00% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	Trastuzumab-emtansine (3 mg/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of SK-OV-3 cells with HER2 expression with high expression.
In Vivo Model	SK-OV-3 CDX model (Expressing YES1 Y537F)
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells (YES1 Y537F expression)		CVCL_0532
Experiment 12 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.50% (Day 48)	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 1 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 13 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.20% (Day 7)	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 3 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 14 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.00% (Day 33)	Positive HER2 expression (HER2+++/++)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 15 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.00% (Day 33)	Moderate HER2 expression (HER2 ++)
Method Description	SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 16 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.50% (Day 21)	Moderate HER2 expression (HER2++)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; JIMT-1 (moderate positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	JIMT-1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 17 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.70% (Day 48)	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 3 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 18 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.00% (Day 58)	Positive HER2 expression (HER2+++/++)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	H3255 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H3255 cells		CVCL_6831
Experiment 19 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.00% (Day 58)	High HER2 expression (HER2 +++)
Method Description	T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks,.
In Vivo Model	H3255 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H3255 cells		CVCL_6831
Experiment 20 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.30% (Day 33)	High HER2 expression (HER2 +++)
Method Description	SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	LS174T CDX model
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 21 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.70% (Day 51)	Low HER2 expression (HER2+)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	HCC827 CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 22 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.00% (Day 7)	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 10 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 23 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.54% (Day 24)	Positive HER2 expression (HER2+++/++)
Method Description	Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (1 mg/kg) via the tail vein on Day 0.    Click to Show/Hide
In Vivo Model	KPL-4 CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 24 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.90% (Day 24)	Positive HER2 expression (HER2+++/++)
Method Description	Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 5 mg/kg) via the tail vein on Day 0.    Click to Show/Hide
In Vivo Model	KPL-4 CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 25 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.90% (Day 10)	High HER2 expression (HER2+++)
Method Description	Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 26 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.39% (Day 24)	Positive HER2 expression (HER2+++/++)
Method Description	Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 1 mg/kg) via the tail vein on Day 0.    Click to Show/Hide
In Vivo Model	KPL-4 CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 27 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.70% (Day 7)	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 15 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 28 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.10% (Day 7)	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 30 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 29 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.70% (Day 48)	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 10 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 30 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.30% (Day 14)	High HER2 expression (HER2+++)
Method Description	KPL-4 human breast tumor cells were inoculated (3 million cells per mouse, in Matrigel) into the mammary fat pads of SCID beige mice. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Trastuzumab-maytansinoid conjugates were given by single 15 mg/kg iv injection.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 31 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70% (Day 48)	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 15 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 32 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.40% (Day 21)	High HER2 expression (HER2+++)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; KPL-4 (strong positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	KPL-4 cell line xenograft model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 33 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 56)	Positive HER2 expression (HER2 +++/++)
Method Description	HER2-positive HCC1954 cells were either treated with vehicle (control) or T-DM1 for 5 days, trypsinized, washed in PBS and sorted by flow cytometry based on the surface ROR1 expression. ROR1- and ROR1+ or unfractionated cells were injected into the subcutaneous site of 6-8-week old Nu/J mice (n=3/group).
In Vivo Model	HCC1954 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 34 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	High HER2 expression (HER2+++)
Method Description	Mice were inoculated subcutaneously in the right flank with either 5x106 cells/mouse of BTC cell line KKU-100, mice were randomized to the control group or treatment with T-DM1 20 mg/kg groups.
In Vivo Model	KMCH-1 CDX model
In Vitro Model	Combined hepatocellular carcinoma and cholangiocarcinoma	KMCH-1 cells		CVCL_7970
Experiment 35 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Minimal Effective Dose (MED)	< 5.00 mg/kg	Moderate HER2 expression (HER2++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: two T-DM1 groups, treated with 20 mg/kg and 60 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 36 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Maximum Tolerated Dose (MTD)	> 20.00 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: two T-DM1 groups, treated with 20 mg/kg and 60 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.98% (Day 7)	High HER2 expression (HER2 +++)
Method Description	An allograft was propagated from the Fo5 mmty transgenic mouse which does not respond to.or responds poorly to HERCEPTIN therapy. Subjects were treated once with ADC (10 mg/kg); and placebo PBS buffer control (Vehicle) andmonitored over 3 weeks.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM±0.12 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.57 nM±0.10 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.76 nM	Moderate HER2 expression (HER2 ++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.71 nM
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 8 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.26 nM	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 9 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.89 nM±3.51 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 10 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.40 nM±4.80 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.37 nM	Low HER2 expression (HER2+; IHC 1+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 12 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 nM	Negative HER2 expression (HER2 -)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 13 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative HER2 expression (HER2 -)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 14 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	220.00 nM±39.50 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 15 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	317.00 nM±93.70 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 16 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 17 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00-15.00 ng/mL	High HER2 expression (HER2+++)
Method Description	Exposing mammalian cells having HER2 receptors to ADC in a cell culture medium; culturing the cells for a period from about 6 hours to about 5 days; and measuring cell viability Cell-based in vitro assays were used to measure viability, cytotoxicity, and induction of apoptosis of the ADC of the invention.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 18 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.00 ug/mL	Negative HER2 expression (HER2-)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 19 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 ug/mL	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 20 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 ug/mL	Positive HER2 expression (HER2+++/++; HER2 MFI=95.7)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 21 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 ug/mL	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 22 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 ug/mL	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 23 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 ug/mL	Low HER2 expression (HER2+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	MKN7 cells		CVCL_1417

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Objective Response Rate (ORR)	12.82%	Positive CD38 expression (CD38+++/++)
Patients Enrolled	Lymphoma limited to diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), mantle cell lymphoma (MCL), or marginal zone lymphoma (MZL). Patients were also required to have received at least one prior anti-CD20 based therapeutic regimen, have a life expectancy of greater than 3 months, an Eastern Cooperative Oncology Group Performance status of 2 or lower, and adequate hematological, renal, and hepatic function.    Click to Show/Hide
Administration Dosage	Conventional 3+3 dose-escalation design; intravenously once every 3 weeks; from 0.10 to 1.80 mg/kg.
Related Clinical Trial
NCT Number	NCT01534715	Clinical Status	Phase 1
Clinical Description	A phase 1, multi-center, open-label study of IMGN529 administered intravenously in adult patients with relapsed or refractory non-Hodgkin lymphoma and chronic lymphocytic leukemia.
Primary Endpoint	A total of five objective responses were observed, resulting in an overall response rate (ORR) of 12.82% (N=39). Four of these (1 complete response [CR] and 3 partial responses [PRs]) occurred in patients with DLBCL, for an ORR of 22% in this lymphoma subset.

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 14.50% (Day 38)	Positive CD38 expression (CD38+++/++)
Method Description	IMGN529 induces efficient tumor cell killing in cell line-derived models B-cell NHL of cells with lower CD27 expression, dosed at 2.5 ug/kg , 2 qw3.
In Vivo Model	CD37-positive NHL and CLL model
In Vitro Model	Non-Hodgkin lymphoma	Non-Hodgkin lymphoma cells		Homo sapiens
	Chronic lymphocytic leukemia	Chronic lymphocytic leukemia cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 38)	Positive CD38 expression (CD38+++/++)
Method Description	IMGN529 induces efficient tumor cell killing in cell line-derived models B-cell NHL of cells with lower CD27 expression, dosed at 5 ug/kg , 2 qw3.
In Vivo Model	CD37-positive NHL and CLL model
In Vitro Model	Non-Hodgkin lymphoma	Non-Hodgkin lymphoma cells		Homo sapiens
	Chronic lymphocytic leukemia	Chronic lymphocytic leukemia cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 38)	Positive CD38 expression (CD38+++/++)
Method Description	IMGN529 induces efficient tumor cell killing in cell line-derived models B-cell NHL of cells with lower CD27 expression, dosed at 10 ug/kg , 2 qw3.
In Vivo Model	CD37-positive NHL and CLL model
In Vitro Model	Non-Hodgkin lymphoma	Non-Hodgkin lymphoma cells		Homo sapiens
	Chronic lymphocytic leukemia	Chronic lymphocytic leukemia cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (10 mg/kg)	Positive CD38 expression (CD38+++/++)
Method Description	The inhibitory activity of SGN-LIV1A against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 1 day.
In Vivo Model	DoHH2 CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-NHL cells		CVCL_1793

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.10 nM
Method Description	In vitro cytotoxicity was measured by incubating 5000 target cells with indicated agents in complete RPMI-1640 media for 5 days at 37°C. The viability of remaining cells was determined by a colorimetric WST-10 assay.
In Vivo Model	DoHH2 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.10 nM
Method Description	In vitro cytotoxicity was measured by incubating 5000 target cells with indicated agents in complete RPMI-1640 media for 5 days at 37°C. The viability of remaining cells was determined by a colorimetric WST-11 assay.
In Vivo Model	DoHH2 CDX model
In Vitro Model	Mantle cell lymphoma	Granta-519 cells		CVCL_1818
Experiment 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.10 nM
Method Description	In vitro cytotoxicity was measured by incubating 5000 target cells with indicated agents in complete RPMI-1640 media for 5 days at 37°C. The viability of remaining cells was determined by a colorimetric WST-8 assay.
In Vivo Model	DoHH2 CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.10 nM	Positive CD38 expression (CD38+++/++)
Method Description	In vitro cytotoxicity was measured by incubating 5000 target cells with indicated agents in complete RPMI-1640 media for 5 days at 37°C. The viability of remaining cells was determined by a colorimetric WST-9 assay.
In Vivo Model	DoHH2 CDX model
In Vitro Model	Diffuse large B-cell lymphoma	Farage cells		CVCL_3302
Experiment 5 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 nM
Method Description	In vitro cytotoxicity was measured by incubating 5000 target cells with indicated agents in complete RPMI-1640 media for 5 days at 37°C. The viability of remaining cells was determined by a colorimetric WST-12 assay.
In Vivo Model	DoHH2 CDX model
In Vitro Model	Mantle cell lymphoma	JVM-2 cells		CVCL_1319

Experiment 1 Reporting the Activity Date of This ADC					[22]
Patients Enrolled	Patients with advanced or metastatic epithelial malignancies.
Administration Dosage	20, 40, 80, 120, 180, and 220 mg/m2 every 3 weeks.
Related Clinical Trial
NCT Number	NCT03094169	Clinical Status	Phase 1/2
Clinical Description	Phase 1a/2a dose escalation trial to determine safety, tolerance, MTD, and preliminary antineoplastic activity of AVID100, in patients with advanced or metastatic solid tumors of epithelial origin.

Experiment 1 Reporting the Activity Date of This ADC					[23]
Related Clinical Trial
NCT Number	NCT03953833	Clinical Status	Phase 1
Clinical Description	Phase 1 clinical trial on the safety, tolerability, pharmacokinetics of B003 in the treatment of HER2-positive recurrent or metastatic breast cancer.

Experiment 1 Reporting the Activity Date of This ADC					[25]
Patients Enrolled	HER2-positive locally advanced or metastatic breast cancer (positivity for HER2 was defined as a score of 2+ in immunohistochemical analysis and a positive result in fluorescence in situ hybridization or a score of 3+ in immunohistochemical analysis), the standard treatment was invalid or there was no effective standard treatment plan, the Eastern Cooperative Oncology Group performance status score was 0-1.    Click to Show/Hide
Administration Dosage	4 dose-escalation sequences, 1.20 mg/kg, 2.40 mg/kg, 3.60 mg/kg and 4.80 mg/kg, once every 21days, as a 90-min intravenous infusion.

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.90% (Day 25)	High CD205 expression (CD205+++; IHC 3+)
Method Description	The antitumor activity of the ADCs was then evaluated in solid and hematologic mouse xenograft models. A total of 5x106-2x107 cells with or without Matrigel, were injected subcutaneously into the flanks of mice. The treatments were started when average tumor volume reached 88-300 mm3. Animals were randomly assigned into groups (6 mice/group), and treated with MEN1309/OBT076 intravenously once weekly for 2 consecutive weeks, 10 mg/kg.    Click to Show/Hide
In Vivo Model	Diffuse Large B-Cell Lymphoma CDX model
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.10% (Day 25)	High CD205 expression (CD205+++; IHC 3+)
Method Description	The antitumor activity of the ADCs was then evaluated in solid and hematologic mouse xenograft models. A total of 5x106-2x107 cells with or without Matrigel, were injected subcutaneously into the flanks of mice. The treatments were started when average tumor volume reached 88-300 mm3. Animals were randomly assigned into groups (6 mice/group), and treated with MEN1309/OBT076 intravenously with a single dose, 10 mg/kg.    Click to Show/Hide
In Vivo Model	Pancreas cancer CDX model
In Vitro Model	Pancreatic cancer	Pancreatic cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive ICAM1 expression (ICAM1+++/++)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.80 nM	Positive ICAM1 expression (ICAM1+++/++)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive ICAM1 expression (ICAM1+++/++)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
In Vitro Model	Normal	hTERT-HPNE cells		CVCL_C466

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 9.18% (Day 44)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.63% (Day 30)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX: CHGA-010)
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.73% (Day 30)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v, q3w x2) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX: CHGA-010)
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.30% (Day 44)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.51% (Day 38)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	MFM223 CDX model
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.93% (Day 22)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.08% (Day 22)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.41% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1-0.7 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast carcinoma	SUM52PE cells		CVCL_3425
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 6 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Negative FGFR2 expression (FGFR2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric carcinoma	NUGC-3 cells		CVCL_1612

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 1 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 5 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 10.40% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 3 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 11.50% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 1 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian cancer	Ovarian cancer cells		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.60% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 5 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian cancer	Ovarian cancer cells		Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.90% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 1 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian adenocarcinoma	OV-90 cells		CVCL_3768
Experiment 7 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.40% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 3 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian cancer	Ovarian cancer cells		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.40% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 3 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian adenocarcinoma	OV-90 cells		CVCL_3768
Experiment 9 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.90% (Day 30)	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 5 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian adenocarcinoma	OV-90 cells		CVCL_3768

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 2.01% (Day 20)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,2 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 12.30% (Day 50)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,1 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.50% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg.    Click to Show/Hide
In Vivo Model	SCLC xenograft model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 4 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.40% (Day 50)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,1 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells		CVCL_0336
Experiment 5 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.30% (Day 60)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3.5 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 6 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.30% (Day 60)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,5 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 7 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.90% (Day 50)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells		CVCL_0336
Experiment 8 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.10% (Day 50)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg. The mice were intraperitoneally administered Etoposide was prepared in dimethyl sulfoxide, and the solution was diluted in PBS just before administration. The mice were intraperitoneally administered etoposide for 2 cycles (3 mg/kg per day;days 15 and days 1115).    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 9 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.30% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg. The mice were intraperitoneally administered Etoposide was prepared in dimethyl sulfoxide, and the solution was diluted in PBS just before administration. The mice were intraperitoneally administered etoposide for 2 cycles (3 mg/kg per day;days 15 and days 1115).    Click to Show/Hide
In Vivo Model	SCLC xenograft model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST-430/654 cells		CVCL_7040
Experiment 3 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.02 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.07 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 5 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 6 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.18 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.52 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 8 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.54 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 9 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.99 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 10 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.71 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung squamous cell carcinoma	NCI-H2170 cells		CVCL_1535
Experiment 11 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.03 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 12 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.30 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 13 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.47 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.38 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Esophageal squamous cell carcinoma	TF-1 cells		CVCL_1759
Experiment 15 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.84 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Normal	COS-7 cells		CVCL_0224
Experiment 16 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.95 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Normal	HUVEC-C cells		CVCL_2959
Experiment 17 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.47 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 18 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.49 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST48 cells		CVCL_7041
Experiment 19 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.63 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	Ms-1 cells		CVCL_IQ55

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 2.05% (Day 22)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.22% (Day 22)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.68% (Day 38)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	MFM223 CDX model
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.61% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast carcinoma	SUM52PE cells		CVCL_3425
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.60 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.70 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.50 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 6 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Negative FGFR2 expression (FGFR2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric carcinoma	NUGC-3 cells		CVCL_1612

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 10.10% (Day 7)	Negative HER2 expression (HER2 -)
Method Description	Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model	MDA-MB-468GFP CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.40% (Day 7)	Negative HER2 expression (HER2 -)
Method Description	Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model	MDA-MB-468GFP CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM - 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Lung squamous cell carcinoma	NCI-H2170 cells		CVCL_1535
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM - 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM - 10 nM	Low HER2 expression (HER2+)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM - 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 5 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.50 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Breast adenocarcinoma	3T3/HER2-luc-GFP cells		Mus musculus
Experiment 6 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Negative HER2 expression (HER2 -)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.58% (Day 49)	Positive ITGAV expression (ITGAV +++/++)
Method Description	The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.12% (Day 28)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.28% (Day 38)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 39.65% (Day 28)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.09% (Day 28)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.00% (Day 41)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75.90% (Day 38)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.25% (Day 38)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.31% (Day 21)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.81% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.0 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.44% (Day 21)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.51% (Day 21)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	59.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	71.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	76.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	80.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	90.00%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	98.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 12 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.55 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 14 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 15 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.82 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	46.83 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 23.23% (Day 27)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (1 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 23.23% (Day 27)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (2 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 38.63% (Day 27)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (4 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 4 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.95% (Day 27)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (8 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 5 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.22% (Day 27)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (16 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 6 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.2% (Day 29)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (30 mg/kg, i.v. injection weekly in a total 4 doses) induces efficient tumor cell killing in cell line-derived models of NCI-H226 cells with CD147 expression with high expression.
In Vivo Model	NCI-H226 CDX model
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 7 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.84% (Day 27)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (32 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 8 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.40% (Day 14)	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (18 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of NCI-H460 cells with CD147 expression with high expression.
In Vivo Model	NCI-H460 CDX model
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 2 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459
Experiment 3 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.96 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566
Experiment 4 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.26 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.74% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 3 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.54% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 6 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.23% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 10 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 4 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.81% (Day 35)	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 15 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.85% (Day 22)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 35.79% (Day 22)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.52% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.00% (Day 14)	Positive KIT expression (KIT+++/++)
Method Description	In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 1 mg/kg twice at day 0 and day 7.
In Vivo Model	Small cell lung cancer CDX model
In Vitro Model	Small cell lung cancer	Small cell lung cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.00% (Day 14)	Positive KIT expression (KIT+++/++)
Method Description	In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 3 mg/kg twice at day 0 and day 7.
In Vivo Model	Small cell lung cancer CDX model
In Vitro Model	Small cell lung cancer	Small cell lung cancer cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.00% (Day 14)	Positive KIT expression (KIT+++/++)
Method Description	In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 5 mg/kg twice at day 0 and day 7.
In Vivo Model	Small cell lung cancer CDX model
In Vitro Model	Small cell lung cancer	Small cell lung cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive KIT expression (KIT+++/++)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 2 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive KIT expression (KIT+++/++)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 3 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.08 nM	Positive KIT expression (KIT+++/++)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 4 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.58 nM	Negative KIT expression (KIT-)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 5 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	35.50 nM	Negative KIT expression (KIT-)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung squamous cell carcinoma	NCI-H2170 cells		CVCL_1535
Experiment 6 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	47.63 nM	Negative KIT expression (KIT-)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Amelanotic melanoma	MDA-MB-435 cells		CVCL_0417

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.00% (Day 23)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 49.00% (Day 40)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.00% (Day 40)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.00% (Day 40)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.00% (Day 40)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	54.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	69.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	69.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	79.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	95.00%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	97.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	100.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 12 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.33 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 15 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.51 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 16 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.69 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.00% (Day 41)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	57.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	70.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	78.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	80.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	90.00%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	98.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 12 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.50 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 14 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.24 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 15 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.07 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	45.43 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.97% (Day 38)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	MFM223 CDX model
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.03% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.69% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 233 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast carcinoma	SUM52PE cells		CVCL_3425
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 6 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Negative FGFR2 expression (FGFR2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric carcinoma	NUGC-3 cells		CVCL_1612

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.00% (Day 41)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 48.00% (Day 20)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3.75 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 20)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 15 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258

Experiment 1 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	Hs 578T cells		CVCL_0332
Experiment 4 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.20 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 6 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.40 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 7 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 8 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 9 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	55.86% (Day 14)	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Animals with established tumors of about 130 mm3 were treated with intravenous single injection of the M9346A-DM conjugates at 25 02 mg/kg, equivalent to 51 3 g conjugated maytansinoid per kg The conjugates were injected on day 7 after cell inoculation.
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.17% (Day 10)	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.01 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00±2.00 nM	Moderate FOLR1 expression (FOLR1++; 290,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure) Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363
Experiment 4 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00±0.70 nM	High FOLR1 expression (FOLR1+++; 1,300,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.67% (Day 20)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 2.5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.15% (Day 20)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.52% (Day 20)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 4 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 5 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 6 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 7 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 nM	Moderate FOLR1 expression (FOLR1 ++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.00% (Day 41)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.61% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.0 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	54.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	69.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	74.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	80.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	91.00%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	98.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 12 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.52 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 14 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.83 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 15 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.22 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.92 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.12% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.61 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.76% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.59 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.65% (Day 42)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.95% (Day 42)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.25% (Day 42)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	65.00% (Day 12)	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	65.00% (Day 12)	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.73% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.12% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.79% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.45 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.86% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.91 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.72% (Day 33)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.00% (Day 41)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.01% (Day 27)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.0 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 23)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 23)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 23)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	53.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	66.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	72.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	78.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	92.00%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	98.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 12 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.72 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.74 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 14 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.26 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 15 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.49 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.77 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.87% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.20 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.02% (Day 30)	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.32% (Day 30)	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg per week (five weeks).
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 3 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.27% (Day 30)	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 450 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124

Experiment 1 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM-1.00 nM	Positive CD138 expression (CD138 +++/++)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD138 expression (CD138 -)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.93% (Day 14)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with Kasumi-1 cells. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	Kasumi-1 CDX model
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.35% (Day 35)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with Kasumi-1 cells. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	HMC-1 CDX model
In Vitro Model	Mast cell leukemia	HMC-1 cells		CVCL_0003
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.00% (Day 43)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 50)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 50)	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	60.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	75.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	86.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	87.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1930 cells		CVCL_1507
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	91.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	CMK-11-5 cells		CVCL_0217
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	92.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	95.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	98.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	OCI-M1 cells		CVCL_2149
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	SKNO-1 cells		CVCL_2196
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Essential thrombocythemia	UKE-1 cells		CVCL_0104
Experiment 12 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	99.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 13 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	100.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Max inhibition rate (MIR)	100.00%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	M-07e cells		CVCL_2106
Experiment 15 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.02 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 16 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	CMK-11-5 cells		CVCL_0217
Experiment 17 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 18 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.08 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	M-07e cells		CVCL_2106
Experiment 19 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.08 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 20 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.09 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1930 cells		CVCL_1507
Experiment 21 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.11 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	OCI-M1 cells		CVCL_2149
Experiment 22 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.15 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 23 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.61 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 24 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	1.29 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 25 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	1.80 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Essential thrombocythemia	UKE-1 cells		CVCL_0104
Experiment 26 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	3.60 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	SKNO-1 cells		CVCL_2196
Experiment 27 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	4.00 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 28 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	4.30 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.60% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	85.00% (Day 12)	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07±0.01 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.56% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	86.67% (Day 12)	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.66% (Day 31)	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3.00 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 20)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of OVCAR-3 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM±0.05 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.54 nM±0.07 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 nM±0.15 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM±0.02 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 nM±0.04 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 nM±0.05 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM±0.04 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.75 nM±0.06 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 nM±0.24 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM±0.01 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 nM±0.15 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.84 nM±0.15 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.42 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.30 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	INA-6 cells		CVCL_5209
Experiment 4 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.80 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	OCI-My7 cells		CVCL_E333
Experiment 5 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.90 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	OCI-My5 cells		CVCL_E332
Experiment 6 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.90 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	KMS-12-BM cells		CVCL_1334
Experiment 7 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.90 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Multiple myeloma	SK-MM-1 cells		CVCL_A478
Experiment 8 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	35.30 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	OPM-2 cells		CVCL_1625
Experiment 9 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37.00 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	JIM3 cells		CVCL_2533
Experiment 10 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.60 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	LP-1 cells		CVCL_0012

Experiment 1 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model	Esophageal adenocarcinoma	OE19 cells		CVCL_1622
Experiment 3 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Normal	HEK293 cells		CVCL_0045
Experiment 2 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 3 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	MMT-060562 cells		CVCL_4241

Experiment 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#10)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#19)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 3 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.41 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.52 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#20)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.68 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#29)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.20 nM	Positive CD19 expression (CD19+++/++)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.60 nM	Negative CD19 expression(CD19-)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.65 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	89.60 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Moderate EGFR expression (EGFR++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 4 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 ng/mL - 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 ng/mL - 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast ductal carcinoma	HCC1143 cells		CVCL_1245
Experiment 4 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.00 ug/mL	Positive CD26 expression (CD26+++/++)
Method Description	Viability assay of Jurkat cells incubated for 72 h with ADC.
In Vitro Model	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Experiment 1 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Disease Control Rate (DCR)	22.60% (31 patients with other tumors) 33.30% (HNSCC) 22.20% (esophageal cancer)
Patients Enrolled	Advanced solid tumors expressing P-cadherin, TNBC, head and neck squamous cell carcinoma (HNSCC), esophageal cancer, cervical cancer, and non-small cell lung cancer (NSCLC).
Administration Dosage	At 10 different dose levels of PCA062, ranging from 0.40 to 5.00 mg/kg every 2 weeks administered as a 1-hour intravenous infusion.
Related Clinical Trial
NCT Number	NCT02375958	Clinical Status	Phase 1
Clinical Description	A phase 1 multi-center, open-label dose escalation and expansion study of PCA062 administered intravenously in adult patients with p-CAD positive tumors.
Primary Endpoint	The MTD was PCA062 3.60 mg/kg every 2 weeks.No patient achieved a complete response. Only 1 patient with stage IV metastatic HNSCC treated at 0.90 mg/kg achieved a confirmed partial response (PR) as best overall response (BOR). The disease control rate (DCR) for the 31 patients with other tumors was 22.60% (95% CI, 9.60-41.10). In patients with HNSCC (n = 6), DCR was 33.30% (95% CI, 4.30-77.70), and in patients with esophageal cancer (n = 9), DCR was 22.20% (95% CI, 2.80-60.00).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[49]
Related Clinical Trial
NCT Number	NCT01963715	Clinical Status	Phase 1
Clinical Description	A phase 1, multi-center, open-label study of IMGN289 administered intravenously in adult patients with EGFR-positive solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Tumor Growth Inhibition value (TGI)	58.30%	High EGFR expression (EGFR+++/++)
Method Description	The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration). IMGN289 dose was 5 mg/kg administered as a single injection.
In Vivo Model	Head and neck squamous cell carcinomas CDX model
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Tumor Growth Inhibition value (TGI)	83.30%	High EGFR expression (EGFR+++/++)
Method Description	The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration). IMGN289 dose was 5 mg/kg administered as a single injection.
In Vivo Model	Head and neck squamous cell carcinomas CDX model
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 3 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Minimal Effective Dose (MED)	1.00 mg/kg	High EGFR expression (EGFR+++/++)
Method Description	The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration).
In Vivo Model	Head and neck squamous cell carcinomas CDX model
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Minimal Effective Dose (MED)	2.50 mg/kg	High EGFR expression (EGFR+++/++)
Method Description	The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration).
In Vivo Model	Head and neck squamous cell carcinomas CDX model
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	High EGFR expression (EGFR+++/++)
Method Description	Effects of IMGN289 on clonogenicity and proliferation were tested in HNSCC cell lines with varying cetuximab and gefitinib sensitivities.
In Vitro Model	Head and neck squamous cell carcinoma	HNSCC cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.30%	Positive KIT expression (KIT+++/++)
Method Description	The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST430 xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628, LMJ729, imatinib.
In Vivo Model	KIT-expressing GIST430 xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.00%	Positive KIT expression (KIT+++/++)
Method Description	The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive NCI-H1048 SCLC xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model	KIT-expressing NCI-H1048 SCLC xenograft model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75.00%	Positive KIT expression (KIT+++/++)
Method Description	The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST430 xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628, LMJ729, imatinib.
In Vivo Model	KIT-expressing GIST430 xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.20%	Positive KIT expression (KIT+++/++)
Method Description	The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST-T1 xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model	KIT-expressing GIST-T1 xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 5 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	82.20%	Positive KIT expression (KIT+++/++)
Method Description	The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST-T1 xenograft model. An efficacy study (single 0.625 mg/kg dose) in the GIST-T1 xenograft model in mice was performed.
In Vivo Model	KIT-expressing GIST-T1 xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 6 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.30%	Positive KIT expression (KIT+++/++)
Method Description	The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive NCI-H1048 SCLC xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model	KIT-expressing NCI-H1048 SCLC xenograft model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.30%	Positive KIT expression (KIT+++/++)
Method Description	The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive NCI-H1048 SCLC xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model	KIT-expressing NCI-H1048 SCLC xenograft model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	< 0.50 nM	Positive KIT expression (KIT+++/++)
Method Description	The inhibitory activity of LOP-628 against cancer cell growth was compared with LMJ729 against cancer cell growth in vitro.
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	< 1.00 nM	Positive KIT expression (KIT+++/++)
Method Description	The inhibitory activity of LOP-628 against cancer cell growth was compared with LMJ729 against cancer cell growth in vitro.
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 3 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	> 10.00 nM	Negative KIT expression (KIT-)
Method Description	The inhibitory activity of LOP-628 against cancer cell growth was compared with LMJ729 against cancer cell growth in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419