Linker ID	LIN0ENDIF
Linker Name	Mc-Val-Ala
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
	3D MOL			2D MOL
Formula	C18H27N3O6
Isosmiles	C[C@@H](C(=O)O)NC(=O)[C@H](C(C)C)NC(=O)CCCCCN1C(=O)C=CC1=O
PubChem CID	67452206
InChI	InChI=1S/C18H27N3O6/c1-11(2)16(17(25)19-12(3)18(26)27)20-13(22)7-5-4-6-10-21-14(23)8-9-15(21)24/h8-9,11-12,16H,4-7,10H2,1-3H3,(H,19,25)(H,20,22)(H,26,27)/t12-,16-/m0/s1
InChIKey	GSWKJIWKGSPISH-LRDDRELGSA-N
IUPAC Name	(2S)-2-[[(2S)-2-[6-(2,5-dioxopyrrol-1-yl)hexanoylamino]-3-methylbutanoyl]amino]propanoic acid
Pharmaceutical Properties	Molecule Weight		381.4	Polar area		133
	Complexity		611	xlogp Value		0.5
	Heavy Count		27	Rot Bonds		11
	Hbond acc		6	Hbond Donor		3

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Partial Response (PR)	4.17%	High EGFR expression (EGFR+++)
Patients Enrolled	Advanced, histologically confirmed solid tumors associated with EGFR overexpression (centralized testing).
Administration Dosage	Ser-T intravenously once every 4 weeks (Q4W; 5-50 ug/kg) in the dose-escalation phase.
Related Clinical Trial
NCT Number	NCT03234712	Clinical Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).
Primary Endpoint	One patient was PR (N=1/24, 4.17%), 6 patients was SD (N=6/24,25.00%). Median DOR (CR + PR + SD)=6.40 months (95% CI 3.0not reached). The median PFS=1.8 months (95% CI 1.3-5.8), median OS=7.10 months (95% CI: 4.1-12.3).
Other Endpoint	Ser-T RP2D regimen=25 ug/kg Q4W.
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Partial Response (PR)	4.20%	High EGFR expression (EGFR+++)
Patients Enrolled	Advanced, histologically confirmed solid tumors associated with EGFR overexpression (centralized testing).
Administration Dosage	Ser-T intravenously once every 4 weeks (Q4W; 5-50 ug/kg) in the dose-escalation phase.
Related Clinical Trial
NCT Number	NCT03234712	Clinical Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).
Primary Endpoint	Responses included 1 partial response (PR), 6 stable disease (SD), 14 progressive disease (PD); 3 patients were not evaluable for response. Median duration of clinical benefit (complete response + PR + SD) was 6.40 months (95% CI: 3.00-not reached).
Other Endpoint	The median PFS was 1.80 months (95% CI: 1.30-5.80) and the median OS was 7.10 months (95% CI: 4.10-12.30).
Experiment 3 Reporting the Activity Date of This ADC					[3]
Related Clinical Trial
NCT Number	NCT03234712	Clinical Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.00% (Day 66)	High EGFR expression (EGFR+++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO199)
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.00% (Day 66)	Low EGFR expression (EGFR+)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO199)
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.00% (Day 24)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,demonstrated with ABBV-321 dosed at 0.15 mg/kg 2 every seven days 3.
In Vivo Model	EGFR-expressing malignant mesothelioma PDX model (PDX: 1174)
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.57% (Day 68)	Moderate EGFR expression (EGFR++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO207)
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.20% (Day 70)	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO199)
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.60% (Day 66)	Moderate EGFR expression (EGFR++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO207)
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.70% (Day 74)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO207)
Experiment 8 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80% (Day 33)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression, administered at 0.5 mg/kg on a Q7D 6 regimen.
In Vivo Model	EGFR-expressing colorectal adenocarcinoma PDX model (PDX: LoVo)
Experiment 9 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.40% (Day 74)	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO207)
Experiment 10 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.20% (Day 70)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO199)

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.40% (Day 28)	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.0125 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.30% (Day 35)	Low EGFR expression (EGFR+)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of lung squamous cell carcinoma cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.60% (Day 28)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.025 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.80% (Day 38)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing A-253 CDX model
In Vitro Model	Submandibular gland squamous cell carcinoma	A-253 cells		CVCL_1060
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.10% (Day 38)	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model	EGFR-expressing A-253 CDX model
In Vitro Model	Submandibular gland squamous cell carcinoma	A-253 cells		CVCL_1060
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.80% (Day 28)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.05 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.80% (Day 28)	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.10% (Day 31)	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing FaDu CDX model
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 9 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.90% (Day 30)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing HCT 116 CDX model
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 10 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.90% (Day 30)	Low EGFR expression (EGFR+)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,administered 0.4 mg/kg,at every seven days 3.
In Vivo Model	EGFR-expressing HCT 116 CDX model
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 11 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.80% (Day 31)	Negative EGFR expression (EGFR-)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model	EGFR-expressing FaDu CDX model
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 12 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	Low EGFR expression (EGFR+)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022
Experiment 13 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	High EGFR expression (EGFR+++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022
Experiment 14 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 42)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022
Experiment 15 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 42)	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022
Experiment 16 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 24)	Low EGFR expression (EGFR+)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of lung squamous cell carcinoma cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model	EGFR-expressing EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.00 pM
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	U-87 MGvIII cells		CVCL_0022
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.10 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SK-CO-1 cells		CVCL_0626
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.40 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	SF268 cells		CVCL_1689
Experiment 8 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.50 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	M059K cells		CVCL_0401
Experiment 9 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.50 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 10 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.80 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW403 cells		CVCL_0545
Experiment 11 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.90 nM	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Primitive neuroectodermal tumor	PFSK-1 cells		CVCL_1642
Experiment 12 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.50 nM	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Gliosarcoma	SF539 cells		CVCL_1691
Experiment 13 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.60 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 201 cells		CVCL_1987
Experiment 14 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.80 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	M059J cells		CVCL_0400
Experiment 15 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.30 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 205 cells		CVCL_0218
Experiment 16 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.70 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	SNB-19 cells		CVCL_0535
Experiment 17 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.30 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 18 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.60 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 19 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.60 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW1116 cells		CVCL_0544
Experiment 20 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.70 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon carcinoma	RKO cells		CVCL_0504
Experiment 21 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.80 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Anaplastic astrocytoma	CHLA-03-AA cells		CVCL_U616
Experiment 22 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.80 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Rectal adenocarcinoma	SW1463 cells		CVCL_1718
Experiment 23 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.50 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	WiDr cells		CVCL_2760
Experiment 24 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW480 cells		CVCL_0546
Experiment 25 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.40 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	LN-18 cells		CVCL_0392
Experiment 26 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	DLD-1 cells		CVCL_0248
Experiment 27 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.50 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Cecum adenocarcinoma	LS1034 cells		CVCL_1382
Experiment 28 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.60 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	SNB-75 cells		CVCL_1706
Experiment 29 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.80 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	T84 cells		CVCL_0555
Experiment 30 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 31 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.90 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	Caco-2 cells		CVCL_0025
Experiment 32 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.50 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556
Experiment 33 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.10 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	U-138MG cells		CVCL_0020
Experiment 34 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.60 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 320DM cells		CVCL_0219
Experiment 35 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Anaplastic astrocytoma	DBTRG-05MG cells		CVCL_1169
Experiment 36 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.20 nM
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	A-172 cells		CVCL_0131
Experiment 37 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.90 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 320HSR cells		CVCL_0220
Experiment 38 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.40 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	HCT 15 cells		CVCL_0292

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Objective Response Rate (ORR)	0.00%
Patients Enrolled	Locally advanced or metastatic solid tumor types associated with PRLR expression, including breast cancer, colorectal cancer, and adrenocortical carcinoma. Patients had progressed on prior treatment, were not amenable to treatment with curative intent, and had no other therapy options known to provide clinical benefit, or were ineligible for such therapies. Patients had an Eastern Cooperative Oncology Group performance status of 0 or 1, and adequate bone marrow, renal, and hepatic function.    Click to Show/Hide
Administration Dosage	Initial dose was 2.70 ug/kg, dose increment was capped at a 100% increase, or at a 50% increase if a grade2 drug-related toxicity had been observed, intravenously every 21 days.
Related Clinical Trial
NCT Number	NCT03145909	Clinical Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics and anti-tumor activity of ABBV-176 in subjects with advanced solid tumors likely to express prolactin receptor (PRLR).
Primary Endpoint	MtD was not formally determined, as identification of a tolerable dose was confounded by late-onset toxicities. ABBV-176 was associated with significant toxicity in this phase 1, dose-escalation study.
Other Endpoint	No patient had an objective response.

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.50%
Method Description	Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.5 mg/kg.
In Vivo Model	BT-474 CDX
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00%
Method Description	Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.1 mg/kg.
In Vivo Model	BT-474 CDX
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00%
Method Description	Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.3 mg/kg.
In Vivo Model	BT-474 CDX
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.50 pM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	CAMA-1 cells		CVCL_1115
Experiment 3 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Prostate carcinoma	22RV1 cells		CVCL_1045
Experiment 4 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Colon adenocarcinoma	SW403 cells		CVCL_0545
Experiment 5 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Ovarian clear cell adenocarcinoma	SMOV-2 cells		CVCL_S920
Experiment 6 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 7 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 8 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.60 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Endometrial adenocarcinoma	AN3-CA cells		CVCL_0028
Experiment 10 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.20 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells		CVCL_0336
Experiment 12 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.60 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Hepatoblastoma	Hep-G2 cells		CVCL_0027
Experiment 13 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 22.00 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma of no special type	UACC-812 cells		CVCL_1781
Experiment 14 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 22.00 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.60% (Day 28)	Positive EGFR expression (EGFR+++/++)
Method Description	For the PDX 14R091 and PDX MPM36 studies, mice received ABBV-322 (0.03 mg/kg) or control ADC (0.03 mg/kg) every 4 days, for a total of 12 treatments.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: MPM36)
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.80% (Day 60)	Positive EGFR expression (EGFR+++/++)
Method Description	For the PDX 14R091 and PDX MPM36 studies, mice received ABBV-322 (0.03 mg/kg) or control ADC (0.03 mg/kg) every 4 days, for a total of 12 treatments.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: 14R091)

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ug/mL - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural biphasic mesothelioma	MSTO-211H cells		CVCL_1430
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ug/mL - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H28 cells		CVCL_1555
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ug/mL - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H2052 cells		CVCL_1518
Experiment 4 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ug/mL - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H2052 cells		CVCL_1518

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	70.68% (Day 36)	Low MET expression (MET+; IHC 1+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0363)
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75.79% (Day 22)	High MET expression (MET+++; IHC 3+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0170)
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.94% (Day 21)	Moderate MET expression (MET++; IHC 2+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0159)

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.94% (Day 32)	Positive MET expression (MET +++/++)
Method Description	Mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype or ADC at 0.3 mg/kg intraperitoneally.
In Vivo Model	SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SK-CO-1 cells		CVCL_0626
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	U-138MG cells		CVCL_0020
Experiment 4 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	M059J cells		CVCL_0400
Experiment 5 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	M059K cells		CVCL_0401
Experiment 6 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Anaplastic astrocytoma	DBTRG-05MG cells		CVCL_1169
Experiment 7 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.90 pM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	HCC15 cells		CVCL_2057
Experiment 9 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	DLD-1 cells		CVCL_0248
Experiment 10 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 11 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 12 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 13 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gliosarcoma	SF264 cells		Homo sapiens
Experiment 14 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW403 cells		CVCL_0545
Experiment 15 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	SNB-19 cells		CVCL_0535
Experiment 16 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 201 cells		CVCL_1987
Experiment 17 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 7.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 18 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High MET expression (MET+++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 19 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon carcinoma	RKO cells		CVCL_0504
Experiment 20 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Rectal adenocarcinoma	SW1463 cells		CVCL_1718
Experiment 21 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	WiDr cells		CVCL_2760
Experiment 22 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High MET expression (MET+++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gastric adenocarcinoma	Hs 746.T cells		CVCL_0333
Experiment 23 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	M059J cells		CVCL_0400
Experiment 24 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Pancreatic carcinoma	KP-4 cells		CVCL_1338
Experiment 25 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung papillary adenocarcinoma	NCI-H820 cells		CVCL_1592
Experiment 26 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	SW900 cells		CVCL_1731
Experiment 27 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 205 cells		CVCL_0218
Experiment 28 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 320DM cells		CVCL_0219
Experiment 29 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW1116 cells		CVCL_0544
Experiment 30 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 31 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Cecum adenocarcinoma	LS1034 cells		CVCL_1382
Experiment 32 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 320HSR cells		CVCL_0220
Experiment 33 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gliosarcoma	SF539 cells		CVCL_1691
Experiment 34 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung adenocarcinoma	NCI-H1573 cells		CVCL_1478
Experiment 35 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 36 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	High MET expression (MET+++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 37 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 38 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 39 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	T84 cells		CVCL_0555
Experiment 40 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630
Experiment 41 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	U-118MG cells		CVCL_0633
Experiment 42 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 43 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 44 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 45 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Anaplastic astrocytoma	CHLA-03-AA cells		CVCL_U616
Experiment 46 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.45 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Primitive neuroectodermal tumor	PFSK-1 cells		CVCL_1642
Experiment 47 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW480 cells		CVCL_0546
Experiment 48 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.20 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	SNB-75 cells		CVCL_1706
Experiment 49 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	Caco-2 cells		CVCL_0025
Experiment 50 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	HCT 15 cells		CVCL_0292
Experiment 51 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	A-172 cells		CVCL_0131
Experiment 52 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	141 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	60.13% (Day 13)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	EBC-1 squamous NSCLC cells (5 million) were implanted subcutaneously into SCID mice, and micewere randomized when the tumors reached 175 mm and dosed with ADC or isotype antibody at 0.6 mg/kg intraperitoneally on day 0.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	73.58% (Day 17)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 0.1 mg/kg intraperitoneally.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 3 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.33% (Day 17)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 0.3 mg/kg intraperitoneally.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 4 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	94.51% (Day 17)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 6 mg/kg intraperitoneally.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 pM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in LRRC15 transfected 3T12 cells by isotype-S239C-PBD-E2 or huM25-S239CPBD-E2. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Squamous non-small cell lung cancer	BALB/3T12-3 cells (huLRRC15 transfection)		CVCL_0637
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM-100.00 Nm	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in A549 cells that have undergone epithelial tomesenchymal transition (EMT) in the presence of 10 ng/mL TGFB by isotype-S239C-PBD-E2huM25-S239C-PBD-E2, or huM25-S239C antibody.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM-100.00 Nm	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in A549 lung cancer cells in the presence of 10 ng/mL TGFB by isotype-S239C-PBD-E2huM25-S239C-PBD-E2, or huM25-S239C antibody.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.90% (Day 30)	High CD276 expression (CD276+++)
Method Description	The in vivo antitumor efficacy and tolerability of the selected NAMPTi-ADCs were evaluated in the cell line-derived THP-1 human AmL xenograft model.Treatment with the low-DAR B7H3-EC3 (5 mg/kg,iv,Q7Dx3).
In Vivo Model	Monocytic leukemia CDX model
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.00% (Day 18)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	EBC-1 squamous NSCLC cells (5 million) were implanted subcutaneously into SCID mice, and mice were randomized when the tumors reached 225 mm and dosed with ADC at 0.6 mg/kg Q7Dx2 (one dose given every 7 days for a total of 2 doses) or isotype antibody at 6 mg/kg intraperitoneally starting on day 0.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95.80% (Day 26)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 adeno NSCLCcells (5 million) were implanted subcutaneously into SCID/Beige mice, and mice were randomized whenthe tumors reached 225 mm and dosed with ADC at 0.6 mg/kg or isotype antibody at 12 mg/kg intraperitoneally once on day 0.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in murine Balb/c BM-MSC (Cyagen) mesenchymal stem cells in thepresence of 10 ng/mL TGF by isotype-PBD-DAR2 or huAD208.4.1-PBD-DAR2. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Normal	Mouse bone marrow-derived mesenchymal stem (BM-MSC) cells		Mus musculus
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM-100.00 Nm	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in human BM-MSC (Lonza) mesenchymalstem cells in the presence of 10 ng/mL TGFB by isotype-PBD-DAR2 or huAD208.4.1-PBD-DAR2. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Normal	Human bone marrow-derived mesenchymal stem (BM-MSC) cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.10% (Day 30)	High HER2 expression (HER2+++)
Method Description	The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.20% (Day 30)	High HER2 expression (HER2+++)
Method Description	The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.40 nM	High HER2 expression (HER2+++)
Method Description	Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	56.10 nM	High HER2 expression (HER2+++)
Method Description	Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	344.60 nM	High HER2 expression (HER2+++)
Method Description	Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50% (Day 30)	High CD276 expression (CD276+++)
Method Description	The in vivo antitumor efficacy and tolerability of the selected NAMPTi-ADCs were evaluated in the cell line-derived THP-1 human AmL xenograft model.Treatment with the high-DAR B7H3-EC3 (DAR 7.8; 5 mg/kg,iv,Q7Dx3).
In Vivo Model	Monocytic leukemia CDX model
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300.00 nM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.10 nM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.00 nM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Incomplete Count Recovery (CRi)	26.00% (Placebo + HMA)
Patients Enrolled	Older patients with newly diagnosed acute myeloid leukemia (AML).
Administration Dosage	33A, iv, 10 mcg/kg, every 4 weeks plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks; placebo plus plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks.
Related Clinical Trial
NCT Number	NCT02326584	Clinical Status	Phase 1
Clinical Description	A phase 1b dose-escalation study of SGN-CD33A in combination with standard-of-care for patients with newly diagnosed acute myeloid leukemia.
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Complete Remission (CR)	66.70% (Pre-allo Before Stem Cell Transplant)
Patients Enrolled	Patients With Relapsed or Refractory AmL.
Administration Dosage	Post-allo after stem cell transplant in Day 1 of each cycle; Pre-allo in Day 1 of each cycle plus melphalan 30 mg/m2/day iv and fludarabine 140 mg/m2 iv before stem cell transplant.
Related Clinical Trial
NCT Number	NCT02785900	Clinical Status	Phase 3
Clinical Description	A randomized, double-blind phase 3 study of vadastuximab talirine (SGN-CD33A) versus placebo in combination with azacitidine or decitabine in the treatment of older patients with newly diagnosed acute myeloid leukemia (AML).
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Complete Remission (CR)	11.00% (all treated, dose escalation/expansion 40 ug/kg) 12.00% (efficacy evaluable, dose escalation/expansion 40 ug/kg) 22.00% (all treated treatment naive 40 ug/kg) 23.00% (efficacy evaluable, treatment naive 40 ug/kg)
Patients Enrolled	CD33-positive AmL (any level of CD33 expression as detected by local flow cytometric assessment) and had either newly diagnosed AmL (declining intensive induction/consolidation chemotherapy) or AmL relapsed after a minimum remission duration of 12 weeks after intensive induction/consolidation.
Administration Dosage	Slow IV push on day 1 (5-60 ug/kg) or on days 1 and 4 (20 ug/kg) of 21-day cycles.
Related Clinical Trial
NCT Number	NCT01902329	Clinical Status	Phase 1
Clinical Description	A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.
Primary Endpoint	The recommended monotherapy dose is 4.00 mg/kg.
Other Endpoint	The complete remission rate (CRc) among the 69 patients in the dose-finding cohorts, was 19.00% (6.00% CR + 13.00% CRi, 95% confidence interval [CI], 10.40-30.10).
Experiment 4 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Complete Remission (CR)	30.00% (33A + HMA) 26.00% (Placebo + HMA)
Patients Enrolled	Older patients with newly diagnosed acute myeloid leukemia (AML).
Administration Dosage	33A, iv, 10 mcg/kg, every 4 weeks plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks; placebo plus plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks.
Related Clinical Trial
NCT Number	NCT02326584	Clinical Status	Phase 1
Clinical Description	A phase 1b dose-escalation study of SGN-CD33A in combination with standard-of-care for patients with newly diagnosed acute myeloid leukemia.
Experiment 5 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Complete Remission (CR)	43.00% (all treated) 42.00% (secondary AmL) 34.00% (75 y old) 80.00% (FLT3/ITD+) 50.00% (MRC adv) 39.00% (Und. Myelo)
Patients Enrolled	New diagnosis of CD33-expressing AmL, they could not have received prior therapy with HMAs; however, prior low-intensity treatment, such as hydroxyurea for cytoreduction or other low-intensity therapies for preceding myelodysplastic syndrome (MDS), an Eastern Cooperative Oncology Group (ECOG) performance status 0 or 1, with adequate baseline renal, hepatic, and pulmonary function.    Click to Show/Hide
Administration Dosage	Azacitidine (75 mg/m2 subcutaneous/intravenous 7 days) or decitabine (20 mg/m2 intravenous 5 days) was administered per institutional standard. On the final day of HMA administration (day 7 of azacitidine treatment and day 5 of decitabine treatment), vadastuximab talirine (10 ug/kg) was administered via slow intravenous push (1-2 mL/min), after infusion of the HMA, as 28-day cycles for up to 4 cycles of treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01902329	Clinical Status	Phase 1
Clinical Description	A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.
Primary Endpoint	The 30- and 60-day mortality rates were 2% and 8%, respectively. No DLTs or infusion-related reactions were observed in the combination cohort of this study.
Other Endpoint	CR and CRi, was 70.00% (43% CR + 26% CRi, 95% CI, 55.70-81.70). Median RFS was 7.70 months (95% CI, 4.90-15.40) with 11.30 months (95% CI, 8.80-13.20) median OS.
Experiment 6 Reporting the Activity Date of This ADC					[15]
Patients Enrolled	Patients with operable HER2-positive primary breast cancer.
Administration Dosage	Anthracycline then Trastuzumab Emtansine and Pertuzumab ; Anthracycline then Trastuzumab, Pertuzumab, and Taxane.
Related Clinical Trial
NCT Number	NCT02614560	Clinical Status	Phase 1/2
Clinical Description	A phase 1/2 study of vadastuximab talirine administered in sequence with allogeneic hematopoietic stem cell transplant in patients with relapsed or refractory acute myeloid leukemia (AML).
Experiment 7 Reporting the Activity Date of This ADC					[16]
Patients Enrolled	Patients With acute myeloid leukemia (AML).
Administration Dosage	SGN-CD33A iv in Day 1 or Days 1 and 4 of each cycle; High dose cytarabine + SGN-CD33A (28-day cycles); Standard dose cytarabine and daunorubicin + SGN-CD33A; standard dose cytarabine and daunorubicin + SGN-CD33A and High dose cytarabine + SGN-CD33A.
Related Clinical Trial
NCT Number	NCT01902329	Clinical Status	Phase 1
Clinical Description	A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 36)	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 29.44% (Day 30)	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 30mcg/kg.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 3 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.77% (Day 36)	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 4 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.95% (Day 38)	Negative CD33 expression (CD33-)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.41% (Day 36)	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 1000mcg/kg.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 6 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.53% (Day 38)	Negative CD33 expression (CD33-)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.99% (Day 30)	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 8 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.99% (Day 40)	Negative CD33 expression (CD33-)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=3,919)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG019		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 ng/mL	Moderate CD33 expression (CD33++; 6,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 3 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG022		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=1,355)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG014		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG023		Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 ng/mL	High CD33 expression (CD33+++; CD33 MFI=10,762)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG018		Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 ng/mL	High CD33 expression (CD33+++; CD33 MFI=11,850)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG015		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 ng/mL	Low CD33 expression (CD33+; CD33 MFI=107)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG003		Homo sapiens
Experiment 9 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.90 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=5,817)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG002		Homo sapiens
Experiment 10 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 11 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 12 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 ng/mL	Negative CD33 expression (CD33-; CD33 MFI=20)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG017		Homo sapiens
Experiment 13 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 ng/mL	Negative CD33 expression (CD33-; CD33 MFI=49)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG001		Homo sapiens
Experiment 14 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Acute myeloid leukemia	SH-1 cells		CVCL_2191
Experiment 15 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	High CD33 expression (CD33+++; CD33 MFI=23,223)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 16 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 17 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 7.50 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Acute myeloid leukemia	SIG-M5 cells		CVCL_1694
Experiment 18 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=1,035)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG008		Homo sapiens
Experiment 19 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Low CD33 expression (CD33+; CD33 MFI=216)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG013		Homo sapiens
Experiment 20 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute monocytic leukemia	U-937 cells		CVCL_0007
Experiment 21 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.00 ng/mL	Low CD33 expression (CD33+; CD33 MFI=299)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG010		Homo sapiens
Experiment 22 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Acute myeloid leukemia	HNT-34 cells		CVCL_2071
Experiment 23 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.00 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=1,184)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG004		Homo sapiens
Experiment 24 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33.00 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=6,598)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG011		Homo sapiens
Experiment 25 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	49.00 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=2,278)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens
Experiment 26 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	61.00 ng/mL	Moderate CD33 expression (CD33++; 7,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Esophageal squamous cell carcinoma	TF-1 cells		CVCL_1759
Experiment 27 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	SH-2 cells		CVCL_2190
Experiment 28 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 110.00 ng/mL	Negative CD33 expression (CD33-; CD33 MFI=0)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG009		Homo sapiens
Experiment 29 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 110.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG020		Homo sapiens
Experiment 30 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 110.00 ng/mL	Low CD33 expression (CD33+; CD33 MFI=353)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG012		Homo sapiens
Experiment 31 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 32 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000.00 ng/mL	Low CD33 expression (CD33+; CD33 MFI=318)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Ovarian clear cell adenocarcinoma	ES-2 cells		CVCL_3509
Experiment 33 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 5000.00 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

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Ref 12	A Randomized, Double-blind Phase 3 Study of Vadastuximab Talirine (SGN-CD33A) Versus Placebo in Combination With Azacitidine or Decitabine in the Treatment of Older Patients With Newly Diagnosed Acute Myeloid Leukemia (AML), NCT02785900
Ref 13	A phase 1 trial of vadastuximab talirine as monotherapy in patients with CD33-positive acute myeloid leukemia. Blood. 2018 Jan 25;131(4):387-396.
Ref 14	A phase 1 trial of vadastuximab talirine combined with hypomethylating agents in patients with CD33-positive AML. Blood. 2018 Sep 13;132(11):1125-1133.
Ref 15	A Phase 1/2 Study of Vadastuximab Talirine Administered in Sequence With Allogeneic Hematopoietic Stem Cell Transplant in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML), NCT02614560
Ref 16	A Phase 1 Trial of SGN-CD33A in Patients With CD33-positive Acute Myeloid Leukemia, NCT01902329
Ref 17	SGN-CD33A: a novel CD33-targeting antibody-drug conjugate using a pyrrolobenzodiazepine dimer is active in models of drug-resistant AML. Blood. 2013 Aug 22;122(8):1455-63.