Payload Information
General Information of This Payload
| Payload ID | PAY0XFQLM |
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|---|---|---|---|---|---|---|
| Name | KSP inhibitor |
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| Synonyms |
KSP inhibitor
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| Target(s) | Kinesin-like protein KIF11 (KIF11) | |||||
| Structure |
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| Formula | C36H45F2N5O8 |
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| Isosmiles | CC(C)(C)C(c1cc(-c2cc(F)ccc2F)cn1Cc1ccccc1)N(CCC(N)C(=O)NCCC(=O)NC(CCC(=O)O)C(=O)O)C(=O)CO |
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| InChI |
InChI=1S/C36H45F2N5O8/c1-36(2,3)33(29-17-23(25-18-24(37)9-10-26(25)38)20-42(29)19-22-7-5-4-6-8-22)43(31(46)21-44)16-14-27(39)34(49)40-15-13-30(45)41-28(35(50)51)11-12-32(47)48/h4-10,17-18,20,27-28,33,44H,11-16,19,21,39H2,1-3H3,(H,40,49)(H,41,45)(H,47,48)(H,50,51)
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| InChIKey |
IPQGHUWDCQTNBL-UHFFFAOYSA-N
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| Pharmaceutical Properties | Molecule Weight |
713.779 |
Polar area |
204.29 |
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Complexity |
51 |
xlogp Value |
3.0476 |
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Heavy Count |
51 |
Rot Bonds |
18 |
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Hbond acc |
8 |
Hbond Donor |
6 |
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Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
TWEAKR-KSPi-ADC1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 80.00% (Day 17) | Positive CTLA4 expression (CTLA4 +++/++) | ||
| Method Description |
To exclude anti-tumor effects based on the agonistic activity of the anti-TWEAKR antibody, a maximum dose of 5 mg/kg biweekly was chosen for investigating the anti-tumor activity of TWEAKR-KSPi-ADC1 in mice bearing CT26 tumors.
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| In Vivo Model | CT26 CDX model | ||||
| In Vitro Model | Colon carcinoma | CT26 cells | CVCL_7254 | ||
References
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