General Information of This Linker
Linker ID
LIN0ZGCUP
Linker Name
CL2A
Linker Type
pH-sensitive linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C50H79N9O16
Isosmiles
C1CC(CCC1CN2C(=O)C=CC2=O)C(=O)NCC3=CN(N=N3)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)COCC(=O)N[C@@H](CCCCN)C(=O)NC4=CC=C(C=C4)CO
PubChem CID
154573757
InChI
InChI=1S/C50H79N9O16/c51-14-2-1-3-44(50(66)54-42-10-6-40(36-60)7-11-42)55-46(62)38-75-37-45(61)52-15-17-67-19-21-69-23-25-71-27-29-73-31-32-74-30-28-72-26-24-70-22-20-68-18-16-58-35-43(56-57-58)33-53-49(65)41-8-4-39(5-9-41)34-59-47(63)12-13-48(59)64/h6-7,10-13,35,39,41,44,60H,1-5,8-9,14-34,36-38,51H2,(H,52,61)(H,53,65)(H,54,66)(H,55,62)/t39?,41?,44-/m0/s1
InChIKey
CJDCJOXHKQMGGB-DBSIFAAZSA-N
IUPAC Name
N-[[1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[2-[2-[[(2S)-6-amino-1-[4-(hydroxymethyl)anilino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]acetyl]amino]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methyl]-4-[(2,5-dioxopyrrol-1-yl)methyl]cyclohexane-1-carboxamide
Pharmaceutical Properties
Molecule Weight
1062.2
Polar area
314
Complexity
1620
xlogp Value
-3
Heavy Count
75
Rot Bonds
44
Hbond acc
19
Hbond Donor
6
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Sacituzumab govitecan [Approved]
Identified from the Human Clinical Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Objective Response Rate (ORR)
21.00%
Patients Enrolled
Patients had histologically locally confirmed measurable HR+/HER2 MBC and 2-4 prior systemic chemotherapy regimens for metastatic disease. (Neo)adjuvant therapy for early-stage disease qualified as one of the required prior chemotherapy regimens if the development of unresectable, locally advanced, or metastatic disease occurred within 12 months of therapy (early relapse). Patients must have previously received at least one taxane, at least one anticancer hormonal treatment, and at least one CDK4/6i.

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Administration Dosage
10 mg/kg intravenously once weekly on day 1 and day 8 every 21 days.
Related Clinical Trial
NCT Number NCT03901339  Clinical Status Phase 3
Clinical Description
Phase 3 study of sacituzumab govitecan (IMMU-132) versus treatment of physician's choice (tpc) in subjects with hormonal receptor-positive (hr+) human epidermal growth factor receptor 2 (HER2) negative metastatic breast cancer (MBC) who have failed at least two prior chemotherapy regimens.
Primary Endpoint
medium PFS=5.50 months.
Other Endpoint
medium OS=13.90 months.
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
31.43%
Patients Enrolled
Patients had metastatic triple-negative breast cancer (mTNBC) that had progressed following 2 prior standard chemotherapy regimens (no upper limit) for unresectable, locally advanced, or metastatic disease, and included a taxane (any setting). Per protocol, patients were also eligible after only one prior regimen in the metastatic setting if their disease recurred within 12 months of completing (neo)adjuvant therapy.

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Administration Dosage
10 mg/kg on days 1 and 8 of 21-day cycles; until progression, unacceptable toxicity, study withdrawal, or death.
Related Clinical Trial
NCT Number NCT02574455  Clinical Status Phase 3
Clinical Description
Analysis of patients without and with an initial triple-negative breast cancer diagnosis in the phase 3 randomized ASCENT study of sacituzumab govitecan in metastatic triple-negative breast cancer.
Primary Endpoint
PFS=4.60 months for patients without TNBC at initial diagnosis PFS=5.70 months for patients with TNBC at initial diagnosis.
Other Endpoint
ORR=31.43%.
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Objective Response Rate (ORR)
35.00%
Patients Enrolled
Patients with metastatic triple-negative breast cancer that was relapsed or refractory to two or more previous standard chemotherapy regimens (no upper limit) for unresectable, locally advanced or metastatic disease; previous therapy had to include a taxane (for any indication). Patients had to have triple-negative breast cancer according to standard American Society of Clinical OncologyCollege of American Pathologists criteria.

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Administration Dosage
Sacituzumab govitecan at a dose of 10 mg per kilogram of body weight intravenously on days 1 and 8 of each 21-day cycle.
Related Clinical Trial
NCT Number NCT02574455  Clinical Status Phase 3
Clinical Description
An international, multi-center, open-label, randomized, phase 3 trial of sacituzumab govitecan versus treatment of physician choice in patients with metastatic triple-negative breast cancer who received at least two prior treatments.
Primary Endpoint
Progression-free survival=5.60 months,(95% CI, 4.30-6.30) with sacituzumab govitecan and 1.70 months (95% CI,1.50 to 2.60) with chemotherapy (hazard ratio for disease progression or death, 0.41; 95% CI, 0.32-0.52).
Other Endpoint
The percentage of patients with an objective response was 35.00% with sacituzumab govitecan and 5.00% with chemotherapy.
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Objective Response Rate (ORR)
38.80%
High TROP2 expression (TROP2+++)
Patients Enrolled
Histologically or cytologically confirmed metastatic triple negative breast cancer (mTNBC); refractory or relapsing after 2 prior standard chemotherapy for unresectable, locally advanced, or metastatic disease, including a taxane (any setting).
Administration Dosage
10 mg/kg intravenously on Days 1 and 8 of each 21-day treatment cycle.
Related Clinical Trial
NCT Number NCT04454437  Clinical Status Phase 2
Clinical Description
A phase IIb, single arm, multicenter trial of sacituzumab govitecan in chinese patients with metastatic triple-negative breast cancer who received at least two prior treatments.
Primary Endpoint
Objective response rate=38.80% (95% CI 28.06-50.30), clinical benefit rate=43.80% (95% CI 32.68-55.30).
Other Endpoint
Median PFS=5.55 months (95% CI 4.14-N/A).
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Objective Response Rate (ORR)
14.00%
Patients Enrolled
Patients 18 years of age with mSCLC who had relapsed or were refractory to at least one prior standard line of therapy for metastatic disease, and with measurable tumors by CT, were enrolled. They were required to have Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1, adequate bone marrow, hepatic and renal function, and other eligibility as described in the phase I trial (25). Previous therapy had to be completed at least 2 weeks before enrollment.

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Administration Dosage
Either 8 or 10 mg/kg i.v. on days 1 and 8 of 21-day cycles.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
OrR=14.00% (17.00% for 10 mg/kg group).
Other Endpoint
The median response duration=5.70 months; the clinical benefit rate (CBR>4 months), 34.00%; median PFS=3.70 months; median OS=7.50 months.
Experiment 6 Reporting the Activity Date of This ADC [6]
Efficacy Data Objective Response Rate (ORR)
17.70% (small-cell lung cancer)
22.20% (endometrial cancer)
9.10% (castrate-resistant prostate cancer)
Patients Enrolled
Patients were >18 years of age with metastatic cancer [cervical, clear-cell renal, CRC, epithelial ovarian, endometrial, esophageal, gastric, hepatocellular, CRPC, pancreatic ductal adenocarcinoma, squamous cell head and neck, thyroid, urothelial (UC) cancer; glioblastoma multiforme; mTNBC or non-mTNBC; and SCLC or NSCLC] who had relapsed after or were refractory to at least one prior standard therapeutic regimen.

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Administration Dosage
Intravenous 8, 10, 12, or 18 mg/kg on days 1 and 8 of 21-day cycles until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Safety and pharmacokinetic parameters with investigator-evaluated objective response rate.
Other Endpoint
Efficacy endpoints included: ORR, which included both confirmed partial response (PR) and complete response (CR).
Experiment 7 Reporting the Activity Date of This ADC [7]
Efficacy Data Objective Response Rate (ORR)
19.00%
Patients Enrolled
Patients 18 years with mNSCLC who had measurable disease and progressed after at least one line of therapy for stage IV disease were enrolled. Requirements included Eastern Cooperative Oncology Group performance status 0 or 1, adequate bone marrow and hepatic and renal function, and other eligibility criteria as described in the phase I trial. Prior systemic therapy had to be completed at least 4 weeks before enrollment.

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Administration Dosage
Doses of 8 or 10 mg/kg were given on days 1 and 8 of 21-day cycles; intravenously.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Safety and objective response rate (ORR).
Other Endpoint
Progression-free survival and overall survival.
Experiment 8 Reporting the Activity Date of This ADC [8]
Efficacy Data Objective Response Rate (ORR)
30.00%
Patients Enrolled
Patients 18 years of age who had mTNBC refractory to or relapsed after at least one standard line of therapy since diagnosis and measurable disease by computed tomography scan (or magnetic resonance imaging). patients had an Eastern Cooperative Oncology Group performance status of 0 or 1, adequate bone marrow, hepatic and renal function, and prior toxicities at study entry of grade 1 by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 4.03. Patients with brain metastasis were excluded, unless treated and without progression, and were not receiving high-dose corticosteroids for at least 4 weeks.

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Administration Dosage
10 mg/kg starting dose on days 1 and 8 of 21-day repeated cycles; intravenously; eight cycles.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Safety and objective response rate.
Other Endpoint
Progression-free survival and overall survival.
Experiment 9 Reporting the Activity Date of This ADC [9]
Efficacy Data Objective Response Rate (ORR)
33.30%
Patients Enrolled
Metastatic triple-negative breast cancer.
Administration Dosage
10 mg per kilogram intravenously on days 1 and 8 of each 21-day cycle until disease progression or unacceptable toxic effects.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Objective response rate=33.3% (95% confidence interval [CI].
Other Endpoint
The median duration of response=7.70 months (95% CI, 4.90 to 10.08),clinical benefit rate = 45.40%.
Experiment 10 Reporting the Activity Date of This ADC [10]
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.14 nM
Method Description
Antibody-dependent cell cytotoxicity (ADCC) against Trop-2-positive and Trop-2-negative EC cell lines was measured in vitro,compared to control ADC (P = 0.014 and P = 0.005).
In Vivo Model Endometrioma PDX model (PDX: END(K)265)
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.18-0.26 nM
Method Description
Two Trop-2 positive (CVX-8, ADX-3), and one Trop-2 negative (ADX-2) cell lines were used. A cell line with a strong Trop-2 expression (CVX-8) was used to test in vivo antitumor activity in xenografts models,in vitro experiments.
In Vitro Model Primary cervical cancer Primary cervical cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.60 nM
Method Description
The inhibitory activity of sacituzumab govitecan govitecan against USC with heterogeneous Trop-2 expression was tested by admixing ARK2 USC cells (i.e., high Trop-2 expression) compared to control ADC (p< 0.05),in vitro.
In Vitro Model Endometrial serous adenocarcinoma USPC-ARK-2 cells CVCL_IV73
Experiment 3 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.02 nM
Method Description
Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.

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In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 4 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.44 nM
Method Description
Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.

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In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.86 nM
Method Description
Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.

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In Vitro Model Prostate carcinoma PC-3 cells CVCL_0035
Experiment 6 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.50 nM
Method Description
Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.

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In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 7 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.90 nM
Method Description
The inhibitory activity of sacituzumab govitecan govitecan against USC with heterogeneous Trop-2 expression was tested by admixing ARK2 USC cells (i.e., high Trop-2 expression) compared to control ADC (p< 0.05),in vitro.
In Vitro Model Endometrial serous adenocarcinoma USPC-ARK-2 cells CVCL_IV73
Experiment 8 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.19 nM
Method Description
Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.

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In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Experiment 9 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.61 nM
Method Description
Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.

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In Vitro Model Lung squamous cell carcinoma SK-MES-1 cells CVCL_0630
Labetuzumab govitecan [Phase 2]
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Patients Enrolled
Relapsed or refractory metastatic colorectal cancer (mCRC) who had received at least one prior irinotecan-containing regimen.
Administration Dosage
Once weekly at 8 and 10 mg/kg, or two times per week at 4 and 6 mg/km on weeks 1 and 2 of 3-week repeated cycles, intravenous.
Related Clinical Trial
NCT Number NCT01605318  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of once or twice weekly IMMU-130 (hMN-14-SN38, antibody-drug conjugate) in patients with colorectal cancer.
Primary Endpoint
The median PFS for all 86 patients was 3.60 months (95% CI,2.00 months to 4.00 months), with 16.8% (14 of 86) remaining progression free for at least 6 months, including three patients who maintained this status for at least 1 year. The median OS was 6.90 months (95% CI, 5.70 months to 7.80 months), with 24.41% (21 of 86) surviving for at least 1 year, including three patients who survived at least 2 years (one for 3 years).

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Other Endpoint
In the regorafenib subset (n = 23), the median PFS and OS were 3.90 and 6.70 months, respectively.
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.23 nM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Experiment 2 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.04 nM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate carcinoma DU145 cells CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
140.00 nM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate cancer MSKCC EF1 cells Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.32 uM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate small cell carcinoma NCI-H660 cells CVCL_1576
Epratuzumab-SN38 [Phase 1]
Revealed Based on the Cell Line Data
Click To Hide/Show 37 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
High CD22 expression (CD22+++; Median fluorescence=145.0)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (133 nmol/L).
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.19 nM
Moderate CD22 expression (CD22++; Median fluorescence=45.9)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (1330 nmol/L).
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 nM
High CD22 expression (CD22+++; Median fluorescence=145.0)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (1330 nmol/L).
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 4 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 nM
Negative CD22 expression (CD22-; Median fluorescence=7.7)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (1330 nmol/L).
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 5 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.38 nM
Negative CD22 expression (CD22-; Median fluorescence=7.7)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 alone.
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 6 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.41 nM
Negative CD22 expression (CD22-; Median fluorescence=7.7)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (133 nmol/L).
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 7 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.46 nM
Negative CD22 expression (CD22-; Median fluorescence=7.7)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (133 nmol/L).
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 8 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.46 nM
Negative CD22 expression (CD22-; Median fluorescence=7.7)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (1330 nmol/L).
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 9 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.50 nM
High CD22 expression (CD22+++; Median fluorescence=145.0)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 alone.
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 10 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.51 nM
Moderate CD22 expression (CD22++; Median fluorescence=40.8)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (1330 nmol/L).
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 11 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.73 nM
Moderate CD22 expression (CD22++; Median fluorescence=40.8)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (133 nmol/L).
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 12 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.81 nM
Low CD22 expression (CD22+; Median fluorescence=11.2)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (133 nmol/L).
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 13 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.83 nM
Low CD22 expression (CD22+; Median fluorescence=11.2)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (1330 nmol/L).
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 14 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.84 nM
High CD22 expression (CD22+++; Median fluorescence=145.0)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (133 nmol/L).
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 15 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.16 nM
Moderate CD22 expression (CD22++; Median fluorescence=45.9)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 + Vmab (133 nmol/L).
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 16 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.16 nM
Low CD22 expression (CD22+; Median fluorescence=11.2)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (1330 nmol/L).
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 17 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.50 nM
High CD22 expression (CD22+++; Median fluorescence=145.0)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (1330 nmol/L).
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 18 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.66 nM
Low CD22 expression (CD22+; Median fluorescence=11.2)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (133 nmol/L).
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 19 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.72 nM
Moderate CD22 expression (CD22++; Median fluorescence=45.9)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 alone.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 20 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.77 nM
Low CD22 expression (CD22+; Median fluorescence=11.2)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 alone.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 21 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.84 nM
Moderate CD22 expression (CD22++; Median fluorescence=40.8)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was Emab-SN-38 alone.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 22 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.21 nM
Moderate CD22 expression (CD22++; Median fluorescence=40.8)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (133 nmol/L).
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 23 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.29 nM
Moderate CD22 expression (CD22++; Median fluorescence=40.8)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (1330 nmol/L).
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 24 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.45 nM
Moderate CD22 expression (CD22++; Median fluorescence=45.9)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (1330 nmol/L).
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 25 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.88 nM
Moderate CD22 expression (CD22++; Median fluorescence=45.9)
Method Description
To assess the prospect for enhanced cytotoxicity when EmabSN-38 is combined with unconjugated anti-CD20 antibody,cells were co-incubated with veltuzumab (anti-CD20 IgG) and increasing concentrations of EmabSN-38. Humanized RS7 (hRS7) anti-Trop-2 is a nonbinding human IgG1. The test drug was EmabSN-38 + hRS7 (133 nmol/L).
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 26 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.52 nM
High CD22 expression (CD22+++; Median fluorescence=145.0)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 27 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.68 nM
Negative CD22 expression (CD22-; Median fluorescence=7.7)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 28 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.22 nM
Low CD22 expression (CD22+; Median fluorescence=22.9)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Experiment 29 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.50 nM
Low CD22 expression (CD22+; Median fluorescence=22.9)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific ADC conjugates against several hematopoietic tumor cell lines. The effect of linkage stability on the cytotoxicity of antibody conjugates as determined by a 4-day MTS assay.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Experiment 30 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.68 nM
Low CD22 expression (CD22+; Median fluorescence=22.9)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model Adult B acute lymphoblastic leukemia RS4;11 cells CVCL_0093
Experiment 31 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.10 nM
Moderate CD22 expression (CD22++; Median fluorescence=45.9)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 32 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.25 nM
Low CD22 expression (CD22+; Median fluorescence=11.2)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 33 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.67 nM
Low CD22 expression (CD22+; Median fluorescence=16.0)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model Childhood B acute lymphoblastic leukemia 697 cells CVCL_0079
Experiment 34 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.70 nM
Moderate CD22 expression (CD22++; Median fluorescence=40.8)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific ADC conjugates against several hematopoietic tumor cell lines. The effect of linkage stability on the cytotoxicity of antibody conjugates as determined by a 4-day MTS assay.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 35 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.92 nM
Moderate CD22 expression (CD22++; Median fluorescence=40.8)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 36 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.20 nM
Moderate CD22 expression (CD22++; Median fluorescence=45.9)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific ADC conjugates against several hematopoietic tumor cell lines. The effect of linkage stability on the cytotoxicity of antibody conjugates as determined by a 4-day MTS assay.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 37 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.65 nM
Low CD205 expression (CD205+; IHC 1+)
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific Emab anti-CD22SN-38 conjugates against several hematopoietic tumor cell lines.
In Vitro Model Burkitt lymphoma MN-60 cells CVCL_1421
M603-SN38 DAR6 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [19]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00% (Day 25) High 5T4 expression (5T4+++)
Method Description
Treated with m603.
In Vivo Model Pancreatic cancer CDX model
In Vitro Model Pancreatic cancer Pancreatic cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [19]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 37.83% (Day 25) High 5T4 expression (5T4+++)
Method Description
Treated with m603-SN38.
In Vivo Model Pancreatic cancer CDX model
In Vitro Model Pancreatic cancer Pancreatic cancer cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.90 nM
High 5T4 expression (5T4+++)
Method Description
Cells in the logarithmic phase of growth were collected and seeded in 96-well plates at a density of 510 3 cells/well and cultured overnight. The culture medium was removed and serial dilution ADCs or naked antibodies were added into the wells of 96-well plates in 200 L medium.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
244.20 nM
Moderate 5T4 expression (5T4++)
Method Description
Cells in the logarithmic phase of growth were collected and seeded in 96-well plates at a density of 510 3 cells/well and cultured overnight. The culture medium was removed and serial dilution ADCs or naked antibodies were added into the wells of 96-well plates in 200 L medium.
In Vitro Model Adult hepatocellular carcinoma Huh-7 cells CVCL_0336
N501-SN38 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [19]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00% (Day 25) High 5T4 expression (5T4+++)
Method Description
Treated with n501.
In Vivo Model Pancreatic cancer CDX model
In Vitro Model Pancreatic cancer Pancreatic cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [19]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 62.93% (Day 25) High 5T4 expression (5T4+++)
Method Description
Treated with n501-SN38.
In Vivo Model Pancreatic cancer CDX model
In Vitro Model Pancreatic cancer Pancreatic cancer cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.90 nM
High 5T4 expression (5T4+++)
Method Description
Cells in the logarithmic phase of growth were collected and seeded in 96-well plates at a density of 510 3 cells/well and cultured overnight. The culture medium was removed and serial dilution ADCs or naked antibodies were added into the wells of 96-well plates in 200 L medium.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
49.80 nM
Moderate 5T4 expression (5T4++)
Method Description
Cells in the logarithmic phase of growth were collected and seeded in 96-well plates at a density of 510 3 cells/well and cultured overnight. The culture medium was removed and serial dilution ADCs or naked antibodies were added into the wells of 96-well plates in 200 L medium.
In Vitro Model Adult hepatocellular carcinoma Huh-7 cells CVCL_0336
Anti-BCMA R347-SG3249 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 16.02% (Day 21) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model JJN-3 CDX model
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
CAC10-GT [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [21]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 67.00% (Day 28) Positive CD30 expression (CD30+++/++)
Method Description
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-GT=10 mg/kg.
In Vivo Model HD CDX model
In Vitro Model Hodgkin's disease L540cy cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [21]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 67.00% (Day 28) Positive CD30 expression (CD30+++/++)
Method Description
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-GT=30mg/kg.
In Vivo Model HD CDX model
In Vitro Model Hodgkin's disease L540cy cells Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
20.00 ng/mL
High CD30 expression (CD30+++; 285,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Precursor T-cell acute lymphoblastic leukemia ALCL cells CVCL_A036
Experiment 4 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
27.00 ng/mL
High CD30 expression (CD30+++; 180,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Anaplastic large cell lymphoma DEL/BVR cells CVCL_1170
Experiment 5 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
79.00 ng/mL
High CD30 expression (CD30+++; 400,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Hodgkin's disease L540cy cells Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
160.00 ng/mL
High CD30 expression (CD30+++; 320,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 7 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
850.00 ng/mL
Low CD30 expression (CD30+; 70,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Anti-BCMA I09-SG3249 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.55% (Day 21) High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model NCI-H929 CDX model
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.16% (Day 21) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model JJN-3 CDX model
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
Experiment 3 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.37% (Day 32) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1S CDX model
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.81 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.55 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.79 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
16.16 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Anti-BCMA L15-SG3249 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.16% (Day 21) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model JJN-3 CDX model
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.37% (Day 32) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1S CDX model
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.35% (Day 21) High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model NCI-H929 CDX model
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Anti-BCMA 15B2WT-SG3249 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.59% (Day 21) High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model NCI-H929 CDX model
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Anti-BCMA 15B2GL-SG3249 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.37% (Day 32) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1S CDX model
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.73% (Day 35) High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 3 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1R CDX model
In Vitro Model Plasma cell myeloma MM1.R cells CVCL_8794
Revealed Based on the Cell Line Data
Click To Hide/Show 14 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.99 nM
High BCMA expression (BCMA+++)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.64 nM
High BCMA expression (BCMA+++)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma MM1.R cells CVCL_8794
Experiment 3 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
14.47 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
16.09 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 5 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
16.80 nM
Moderate BCMA expression (BCMA++)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 6 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
22.86 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 7 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
29.12 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 8 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
31.40 nM
Low BCMA expression (BCMA+)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma L-363 cells CVCL_1357
Experiment 9 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
36.28 nM
Moderate BCMA expression (BCMA++)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
Experiment 10 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
39.00 nM
Moderate BCMA expression (BCMA++)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma U266B1 cells CVCL_0566
Experiment 11 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
153.00 nM
High BCMA expression (BCMA+++)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma EJM cells CVCL_2030
Experiment 12 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
201.00 nM
Moderate BCMA expression (BCMA++)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model Plasma cell myeloma OPM-2 cells CVCL_1625
Experiment 13 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500.00 nM Negative BCMA expression (BCMA-)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 14 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500.00 nM Negative BCMA expression (BCMA-)
Method Description
Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model T acute lymphoblastic leukemia Jurkat cells CVCL_0065
H00-GT [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
19.00 ng/mL
High CD30 expression (CD30+++; 285,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Precursor T-cell acute lymphoblastic leukemia ALCL cells CVCL_A036
Experiment 2 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
25.00 ng/mL
High CD30 expression (CD30+++; 180,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Anaplastic large cell lymphoma DEL/BVR cells CVCL_1170
Experiment 3 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
46.00 ng/mL
High CD30 expression (CD30+++; 400,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Hodgkin's disease L540cy cells Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
160.00 ng/mL
High CD30 expression (CD30+++; 320,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 5 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
820.00 ng/mL
Low CD30 expression (CD30+; 70,000 CD30 molecules/cell)
Method Description
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.

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In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Anti-BCMA J6M0-SG3249 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.82 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12.83 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
32.26 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
92.92 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
40H3-CL2A-SN38 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [22]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
19.71 nM
High EGFR expression (EGFR+++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC [22]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
27.83 nM
High EGFR expression (EGFR+++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [22]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
98.81 nM
Moderate EGFR expression (EGFR++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Invasive breast carcinoma of no special type BT-20 cells CVCL_0178
Experiment 4 Reporting the Activity Date of This ADC [22]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100.00 nM Negative EGFR expression (EGFR-)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Veltuzumab-SN-38 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 12 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.83 nM
Moderate CD20 expression (CD20++)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.98 nM
High CD20 expression (CD20+++)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50)
4.88 nM
High CD20 expression (CD20+++)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50)
13.56 nM
High CD20 expression (CD20+++)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 nM High CD20 expression (CD20+++)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 6 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 nM Low CD20 expression (CD20+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Experiment 7 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 nM Low CD20 expression (CD20+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Childhood B acute lymphoblastic leukemia 697 cells CVCL_0079
Experiment 8 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 nM Low CD20 expression (CD20+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Adult B acute lymphoblastic leukemia RS4;11 cells CVCL_0093
Experiment 9 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 nM Low CD20 expression (CD20+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Burkitt lymphoma MN-60 cells CVCL_1421
Experiment 10 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50)
77.90 nM
Moderate CD22 expression (CD22++)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Experiment 11 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50)
162 nM
Low CD20 expression (CD20+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Experiment 12 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Effective Concentration (EC50)
246.60 nM
High CD20 expression (CD20+++)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
References
Ref 1 Sacituzumab Govitecan in Hormone Receptor-Positive/Human Epidermal Growth Factor Receptor 2-Negative Metastatic Breast Cancer. J Clin Oncol. 2022 Oct 10;40(29):3365-3376.
Ref 2 Analysis of patients without and with an initial triple-negative breast cancer diagnosis in the phase 3 randomized ASCENT study of sacituzumab govitecan in metastatic triple-negative breast cancer. Breast Cancer Res Treat. 2022 Sep;195(2):127-139.
Ref 3 Sacituzumab Govitecan in Metastatic Triple-Negative Breast Cancer. N Engl J Med. 2021 Apr 22;384(16):1529-1541.
Ref 4 A Phase IIb, single arm, multicenter trial of sacituzumab govitecan in Chinese patients with metastatic triple-negative breast cancer who received at least two prior treatments. Int J Cancer. 2023 May 15;152(10):2134-2144. doi: 10.1002/ijc.34424. Epub 2023 Jan 30.
Ref 5 Therapy of Small Cell Lung Cancer (SCLC) with a Topoisomerase-I-inhibiting Antibody-Drug Conjugate (ADC) Targeting Trop-2, Sacituzumab Govitecan. Clin Cancer Res. 2017 Oct 1;23(19):5711-5719.
Ref 6 Sacituzumab govitecan, a Trop-2-directed antibody-drug conjugate, for patients with epithelial cancer: final safety and efficacy results from the phase I/II IMMU-132-01 basket trial. Ann Oncol. 2021 Jun;32(6):746-756.
Ref 7 Therapy of Advanced Non-Small-Cell Lung Cancer With an SN-38-Anti-Trop-2 Drug Conjugate, Sacituzumab Govitecan. J Clin Oncol. 2017 Aug 20;35(24):2790-2797.
Ref 8 Efficacy and Safety of Anti-Trop-2 Antibody Drug Conjugate Sacituzumab Govitecan (IMMU-132) in Heavily Pretreated Patients With Metastatic Triple-Negative Breast Cancer. J Clin Oncol. 2017 Jul 1;35(19):2141-2148.
Ref 9 Sacituzumab Govitecan-hziy in Refractory Metastatic Triple-Negative Breast Cancer. N Engl J Med. 2019 Feb 21;380(8):741-751.
Ref 10 Sacituzumab govitecan (IMMU-132), an anti-Trop-2-SN-38 antibody-drug conjugate for the treatment of diverse epithelial cancers: Safety and pharmacokinetics. Cancer. 2017 Oct 1;123(19):3843-3854.
Ref 11 Sacituzumab govitecan, an antibody-drug conjugate targeting trophoblast cell-surface antigen 2, shows cytotoxic activity against poorly differentiated endometrial adenocarcinomas invitro and invivo. Mol Oncol. 2020 Mar;14(3):645-656.
Ref 12 Cervical carcinomas that overexpress human trophoblast cell-surface marker (Trop-2) are highly sensitive to the antibody-drug conjugate sacituzumab govitecan. Sci Rep. 2020 Jan 22;10(1):973.
Ref 13 Clinicopathological features of women with epithelial ovarian cancer and double heterozygosity for BRCA1 and BRCA2: A systematic review and case report analysis. Gynecol Oncol. 2020 Feb;156(2):377-386.
Ref 14 Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69.
Ref 15 Invitro and invivo activity of sacituzumab govitecan, an antibody-drug conjugate targeting trophoblast cell-surface antigen 2 (Trop-2) in uterine serous carcinoma. Gynecol Oncol. 2020 Feb;156(2):430-438.
Ref 16 Phase I/II Trial of Labetuzumab Govitecan (Anti-CEACAM5/SN-38 Antibody-Drug Conjugate) in Patients With Refractory or Relapsing Metastatic Colorectal Cancer. J Clin Oncol. 2017 Oct 10;35(29):3338-3346.
Ref 17 Regulation of CEACAM5 and Therapeutic Efficacy of an Anti-CEACAM5-SN38 Antibody-drug Conjugate in Neuroendocrine Prostate Cancer. Clin Cancer Res. 2021 Feb 1;27(3):759-774.
Ref 18 Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematologic malignancies. Mol Cancer Ther. 2012 Jan;11(1):224-34.
Ref 19 A highly stable human single-domain antibody-drug conjugate exhibits superior penetration and treatment of solid tumors. Mol Ther. 2022 Aug 3;30(8):2785-2799.
Ref 20 Bcma monoclonal antibody-drug conjugate.
Ref 21 Development of Novel Antibody-Camptothecin Conjugates. Mol Cancer Ther. 2021 Feb;20(2):329-339.
Ref 22 Antibody drug conjugates, targeting cancer-expressed EGFR, exhibit potent and specific antitumor activity. Biomed Pharmacother. 2023 Jan;157:114047.
Ref 23 Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematologic malignancies. Mol Cancer Ther. 2012 Jan;11(1):224-34. doi: 10.1158/1535-7163.MCT-11-0632. Epub 2011 Oct 28.

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