Payload Information

General Information of This Payload
Payload ID
PAY0LNGCJ
Name
PBD dimer 13c
Synonyms
PBD dimer 13c
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Target(s) Human Deoxyribonucleic acid (hDNA)
 Target Info 
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
FOLR1-ADC 15 [Investigative]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.60% (Day 95) Low FOLR1 expression (FOLR1+)
Method Description
SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 0.7 mg/kg.
In Vivo Model Ovarian cancer PDX model (PDX: OV90)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.27% (Day 95) Low FOLR1 expression (FOLR1+)
Method Description
SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 1.4 mg/kg.
In Vivo Model Ovarian cancer PDX model (PDX: OV90)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) Low FOLR1 expression (FOLR1+)
Method Description
SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 0.7 mg/kg.
In Vivo Model Ovarian cancer PDX model (PDX: OV90)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) Low FOLR1 expression (FOLR1+)
Method Description
SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 1.4 mg/kg.
In Vivo Model Ovarian cancer PDX model (PDX: OV90)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) Low FOLR1 expression (FOLR1+)
Method Description
SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 2.7 mg/kg.
In Vivo Model Ovarian cancer PDX model (PDX: OV90)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 95) Low FOLR1 expression (FOLR1+)
Method Description
SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 2.7 mg/kg.
In Vivo Model Ovarian cancer PDX model (PDX: OV90)
FOLR1-ADC 13c [Investigative]
 ADC Info 
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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
20.00 pM
Positive FOLR1 expression (FOLR1+++/++)
Method Description
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Negative FOLR1 expression (FOLR1-)
Method Description
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
References
Ref 1 Synthesis of Highly Potent N-10 Amino-Linked DNA-Alkylating Indolinobenzodiazepine Antibody-Drug Conjugates (ADCs). ACS Med Chem Lett. 2019 Jul 22;10(8):1211-1215. doi: 10.1021/acsmedchemlett.9b00254. eCollection 2019 Aug 8.

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