Payload Information

General Information of This Payload
Payload ID
PAY0EKUNN
Name
SG3200
Synonyms
SG3200
   Click to Show/Hide
Target(s) Human Deoxyribonucleic acid (hDNA)
 Target Info 
Structure
Formula
C31H32N4O6
Isosmiles
C=C1CC2C=Nc3cc(OCCCOc4cc5c(cc4OC)C(=O)N4CC(=C)CC4C=N5)c(OC)cc3C(=O)N2C1
InChI
InChI=1S/C31H32N4O6/c1-18-8-20-14-32-24-12-28(26(38-3)10-22(24)30(36)34(20)16-18)40-6-5-7-41-29-13-25-23(11-27(29)39-4)31(37)35-17-19(2)9-21(35)15-33-25/h10-15,20-21H,1-2,5-9,16-17H2,3-4H3
InChIKey
RWZVMMQNDHPRQD-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
556.619
Polar area
102.26
Complexity
41
xlogp Value
4.5249
Heavy Count
41
Rot Bonds
8
Hbond acc
8
Hbond Donor
0
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Trastuzumab-C239I-SG3400 [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 [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 40.50% (Day 50) Negative expression (HER2-)
Method Description
The antitumor activity of trastuzumab-C239i-SG3400 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model Breast cancer CDX model
In Vitro Model Breast cancer Breast cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 48.00% (Day 50) Low HER2 expression (HER2+)
Method Description
The antitumor activity of trastuzumab-C239i-SG3400 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model Gastric cancer CDX model
In Vitro Model Gastric cancer Gastric cancer cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.70 ng/mL
Low HER2 expression (HER2+)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
20.90 ng/mL
Low HER2 expression (HER2+)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
23.30 ng/mL
Low HER2 expression (HER2+)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50.00 ng/mL Negative expression (HER2-)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 250.00 ng/mL Negative expression (HER2-)
Method Description
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
References
Ref 1 Synthesis and evaluation of pyrrolobenzodiazepine dimer antibody-drug conjugates with dual -glucuronide and dipeptide triggers. Eur J Med Chem. 2019 Oct 1;179:591-607.

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