An inhibitor of ATR (Ki = 50 = 19 nM in pancreatic cancer cells in vitro); reduces the IC50 of SN-38 by at least 8-fold in vitro when used at a concentration of 80 nM; delays the growth of radiation-treated PSN-1 pancreatic cancer xenografts in mice by 2-3-fold relative to radiation alone (60 mg/kg); enhances the tumoricidal effects of cisplatin against primary human lung cancer xenografts; enhances the effects of irinotecan against COLO 205 colorectal tumors

VE-822 – 25 mg

Brand:
Cayman
CAS:
1232416-25-9
Storage:
-20
UN-No:
Non-Hazardous - /

VE-822 is an inhibitor of ataxia-telangiectasia mutated (ATM) Rad3-related protein kinase (ATR), a regulator of DNA damage repair, with Ki and IC50 values of in vitro.{36517} It is selective for ATR over ATM (Ki = 34 nM; IC50 = 2,600 nM) as well as DNA-PK, mTOR, and PI3Kγ (Kis = >4,000, >1,000, and 220 nM, respectively). In cultured COLO 205 colorectal cancer cells, VE-822 (80 nM) reduces the IC50 of the topoisomerase 1 inhibitor SN-38 (Item No. 15632) by at least 8-fold.{36519} In a mouse xenograft model, it delays the growth of radiation-treated PSN-1 pancreatic cancer xenografts by 2-3-fold relative to radiation alone when administered at a dose of 60 mg/kg. VE-822 also enhances the tumoricidal effects of cisplatin (Item No. 13119) against primary human lung cancer xenografts and the effects of the topoisomerase inhibitor irinotecan (Item No. 14180) against COLO 205 colorectal tumors in mice.{36519,36518}  

 

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Description

An inhibitor of ATR (Ki = 50 = 19 nM in pancreatic cancer cells in vitro); reduces the IC50 of SN-38 by at least 8-fold in vitro when used at a concentration of 80 nM; delays the growth of radiation-treated PSN-1 pancreatic cancer xenografts in mice by 2-3-fold relative to radiation alone (60 mg/kg); enhances the tumoricidal effects of cisplatin against primary human lung cancer xenografts; enhances the effects of irinotecan against COLO 205 colorectal tumors

Formal name: 3-[3-[4-[(methylamino)methyl]phenyl]-5-isoxazolyl]-5-[4-[(1-methylethyl)sulfonyl]phenyl]-2-pyrazinamine

Synonyms:  VX-970

Molecular weight: 463.6

CAS: 1232416-25-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling||Research Area|Cancer|DNA Damage and Repair

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