Payload Information

General Information of This Payload
Payload ID
PAY0IJSCK
Name
PBD dimer
Synonyms
PBD dimer; SGD-1882; 1222490-34-7; IRE1I9FE08; (6aS)-3-[3-[[(6aS)-2-methoxy-8-(4-methoxyphenyl)-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-8-(4-aminophenyl)-2-methoxy-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one; J3.194.362K; 5H-Pyrrolo(2,1-C)(1,4)benzodiazepin-5-one, 2-(4-aminophenyl)-8-(3-(((11aS)-5,11a-dihydro-7-methoxy-2-(4-methoxyphenyl)-5-oxo-1H-pyrrolo(2,1-C)(1,4)benzodiazepin-8-yl)oxy)propoxy)-1,11a-dihydro-7-methoxy-, (11aS)-; 5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one, 2-(4-aminophenyl)-8-[3-[[(11aS)-5,11a-dihydro-7-methoxy-2-(4-methoxyphenyl)-5-oxo-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy]propoxy]-1,11a-dihydro-7-methoxy-, (11aS)-; 8-(3-((2-(4-Aminophenyl)-7-methoxy-5-oxo-1,11abeta-dihydro-5H-pyrrolo(2,1-C)(1,4)benzodiazepine-8-yl)oxy)propoxy)-7-methoxy-2-(4-methoxyphenyl)-1,11abeta-dihydro-5H-pyrrolo(2,1-C)(1,4)benzodiazepine-5-one; 8-[3-[[2-(4-Aminophenyl)-7-methoxy-5-oxo-1,11abeta-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-8-yl]oxy]propoxy]-7-methoxy-2-(4-methoxyphenyl)-1,11abeta-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one; UNII-IRE1I9FE08; SCHEMBL2291136; OMRPLUKQNWNZAV-CONSDPRKSA-N; EX-A6227; SGD 1882; CS-7766; BP-29355; MS-31248; PD126348; HY-101127; Q27280866; (S)-2-(4-aminophenyl)-7-methoxy-8-(3-((S)-7-methoxy-2-(4-methoxyphenyl)-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-8-yloxy)propoxy)-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5(11aH)-one; 8-(3-((2-(4-AMINOPHENYL)-7-METHOXY-5-OXO-1,11A.BETA.-DIHYDRO-5H-PYRROLO(2,1-C)(1,4)BENZODIAZEPINE-8-YL)OXY)PROPOXY)-7-METHOXY-2-(4-METHOXYPHENYL)-1,11A.BETA.-DIHYDRO-5H-PYRROLO(2,1-C)(1,4)BENZODIAZEPINE-5-ONE
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Target(s) Human Deoxyribonucleic acid (hDNA)
 Target Info 
Structure
Formula
C42H39N5O7
Isosmiles
COC1=CC=C(C=C1)C2=CN3[C@@H](C2)C=NC4=CC(=C(C=C4C3=O)OC)OCCCOC5=C(C=C6C(=C5)N=C[C@@H]7CC(=CN7C6=O)C8=CC=C(C=C8)N)OC
PubChem CID
45257190
InChI
InChI=1S/C42H39N5O7/c1-50-32-11-7-26(8-12-32)28-16-31-22-45-36-20-40(38(52-3)18-34(36)42(49)47(31)24-28)54-14-4-13-53-39-19-35-33(17-37(39)51-2)41(48)46-23-27(15-30(46)21-44-35)25-5-9-29(43)10-6-25/h5-12,17-24,30-31H,4,13-16,43H2,1-3H3/t30-,31-/m0/s1
InChIKey
OMRPLUKQNWNZAV-CONSDPRKSA-N
IUPAC Name
(6aS)-3-[3-[[(6aS)-2-methoxy-8-(4-methoxyphenyl)-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-8-(4-aminophenyl)-2-methoxy-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one
Pharmaceutical Properties
Molecule Weight
725.8
Polar area
138
Complexity
1470
xlogp Value
3.9
Heavy Count
54
Rot Bonds
11
Hbond acc
10
Hbond Donor
1
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) <0.02 mg/L
MCF-7 cells
Invasive breast carcinoma
CVCL_0031 
[1]
Half Maximal Inhibitory Concentration (IC50) <0.02 mg/L
A2780 cells
Ovarian endometrioid adenocarcinoma
CVCL_0134 
[1]
Half Maximal Inhibitory Concentration (IC50) 0.08-0.16 mg/L
WI-38 cells
Normal
CVCL_0579 
[1]
Half Maximal Inhibitory Concentration (IC50) 34.67 nM
Daudi cells
Burkitt lymphoma
CVCL_0008 
[2]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
ABBV-322 [Investigative]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
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 [3]
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)
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 [3]
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 [3]
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 [3]
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 [3]
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
ABT-700 (S238C)-PBD [Investigative]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
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 [4]
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 [4]
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)
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 [4]
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
Revealed Based on the Cell Line Data
Click To Hide/Show 52 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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 [4]
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
D3-GPC2-PBD [Investigative]
 ADC Info 
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 [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.80% (Day 2) High GPC2 expression (GPC2+++)
Method Description
Tumors were typically implanted into the flanks of female 5-9 week-old C.B-17 scid mice. Each mouse was then given a single dose of their respective ADC treatments in PBS or vehicle (Day 0) via intraperitoneal (IP) injection. In some efficacy studies, one cohort of mice received 3 subsequent ADC 1 mg/kg IP injections over the following 2 weeks (1 mg/kg x 4 cohort).

   Click to Show/Hide
In Vivo Model COG-N-421x PDX model
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 [8]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 pM
High GPC2 expression (GPC2+++)
Method Description
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model Neuroblastoma SK-N-AS cells CVCL_1700
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
26.60 pM
Positive GPC2 expression (GPC2 +++/++)
Method Description
Cell lines were plated in 96-well plates (typically between 1,000 and 5,000 cells/well) and treated with serial dilutions of each ADC payload, the D3-GPC2-PBD ADC, or vehicle the following day. After four additional days, cell viability was determined using a CellTiter-Glo Assay.
In Vitro Model Neuroblastoma NB-SD cells CVCL_LF68
HuM25-S239C-PBD-E2 [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
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 [6]
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 [6]
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 [6]
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
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
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 [6]
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 [6]
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
Anti-ApoD PBD [Investigative]
 ADC Info 
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 [7]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.00% Positive APOD expression (APOD +++/++)
Method Description
Male Bl6 mice, at 9 weeks old (young) or 80 weeks old (old), were intravenously treated with the vehicle alone or with anti-ApoD antibody and PBD-conjugated IgG with a cleavable linker, each at a concentration of 0.3 mg/kg and 3 mg/kg in a single dose.
In Vivo Model NHDF CDX model
In Vitro Model Normal NHDF cells Homo sapiens
HuAD208.4.1-PBD-DAR2 [Investigative]
 ADC Info 
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 [6]
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 [6]
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
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 [6]
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 [6]
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
SGN-CD70A [Terminated in phase 2]
 ADC Info 
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 [10]
Efficacy Data Objective Response Rate (ORR)
20.00%
Positive CD70 expression (CD70+++/++)
Patients Enrolled
CD70-positive MCL or DLBCL including FL3b (expression in at least 50% of the sample)
Administration Dosage
8 mg/kg (up to a maximum of 200 mg) intravenously once every 3 weeks.
Related Clinical Trial
NCT Number NCT02216890  Phase Status Phase 1
Clinical Description
Safety study of SGN-CD70A in cancer patients.
Primary Endpoint
Objective response rate=20.00% (95% CI 5.70-43.70).
Other Endpoint
Median progression free survival=1.90 months.
References
Ref 1 Antistaphylococcal activity of DNA-interactive pyrrolobenzodiazepine (PBD) dimers and PBD-biaryl conjugates. J Antimicrob Chemother. 2012 Jul;67(7):1683-96.
Ref 2 ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies. Blood. 2018 Mar 8;131(10):1094-1105.
Ref 3 Targeting and Efficacy of Novel mAb806-Antibody-Drug Conjugates in Malignant Mesothelioma. Pharmaceuticals (Basel). 2020 Oct 2;13(10):289. doi: 10.3390/ph13100289.
Ref 4 ANTI-cMet antibody drug conjugates and methods for their use; 2017-11-23.
Ref 5 A GPC2 antibody-drug conjugate is efficacious against neuroblastoma and small-cell lung cancer via binding a conformational epitope. Cell Rep Med. 2021 Jul 21;2(7):100344.
Ref 6 Anti-huLRRC15 antibody drug conjugates and methods for their use. 2017-06-08
Ref 7 New Senolysis Approach via Antibody-Drug Conjugate Targeting of the Senescent Cell Marker Apolipoprotein D for Skin Rejuvenation. Int J Mol Sci. 2023 Mar 20;24(6):5857. doi: 10.3390/ijms24065857.
Ref 8 A GPC2 antibody-drug conjugate is efficacious against neuroblastoma and small-cell lung cancer via binding a conformational epitope. Cell Rep Med. 2021 Jul 21;2(7):100344. doi: 10.1016/j.xcrm.2021.100344.
Ref 9 Antibody-Drug Conjugate Efficacy in Neuroblastoma: Role of Payload, Resistance Mechanisms, Target Density, and Antibody Internalization. Mol Cancer Ther. 2021 Nov;20(11):2228-2239. doi: 10.1158/1535-7163.MCT-20-1034.
Ref 10 A phase 1 trial of SGN-CD70A in patients with CD70-positive diffuse large B cell lymphoma and mantle cell lymphoma. Invest New Drugs. 2019 Apr;37(2):297-306. doi: 10.1007/s10637-018-0655-0. Epub 2018 Aug 22.

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