Payload Information

General Information of This Payload
Payload ID
PAY0PDMRA
Name
TLR7 agonist-1
Synonyms
TLR7 agonist-1
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Target(s) Toll-like receptor 7 (TLR7)
 Target Info 
Structure
Formula
C21H23N5
Isosmiles
CCCCc1nc2c(N)nc3ccccc3c2n1Cc1ccc(N)cc1
InChI
InChI=1S/C21H23N5/c1-2-3-8-18-25-19-20(16-6-4-5-7-17(16)24-21(19)23)26(18)13-14-9-11-15(22)12-10-14/h4-7,9-12H,2-3,8,13,22H2,1H3,(H2,23,24)
InChIKey
XURWVKISYBUGHB-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
345.45
Polar area
82.75
Complexity
26
xlogp Value
4.1398
Heavy Count
26
Rot Bonds
5
Hbond acc
5
Hbond Donor
2
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
IFNalpha induction level ≈252 pg/mL
Human peripheral blood mononuclear cells(hPBMCs)
Normal
CVCL_0140 
[1]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Anti-HER2_vc-1 [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 [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.20% (Day 30) High HER2 expression (HER2+++)
Method Description
Approximately 2 million cells (100 L of the mixture) were implanted subcutaneously to the right flank of 68 weeks old female SCID/beige mice. After the tumors reached about 200 to 400 mm3 ,the mice were treated with either anti-HER2_vc-1 or non-targeted ADC at 3 mpk (IP,Q5dx3).
In Vivo Model Breast cancer CDX model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 30) High HER2 expression (HER2+++)
Method Description
Approximately 2 million cells (100 L of the mixture) were implanted subcutaneously to the right flank of 68 weeks old female SCID/beige mice. After the tumors reached about 200 to 400 mm3 ,the mice were treated with either anti-HER2_vc-1 or non-targeted ADC at 10 mpk (IP,Q5dx3).
In Vivo Model Breast cancer CDX model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
References
Ref 1 Design and Characterization of Immune-Stimulating Imidazo[4,5-c]quinoline Antibody-Drug Conjugates. Mol Pharm. 2022 Sep 5;19(9):3228-3241.
Ref 2 Design and Characterization of Immune-Stimulating Imidazo[4,5-c]quinoline Antibody-Drug Conjugates. Mol Pharm. 2022 Sep 5;19(9):3228-3241.

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