Cas No.: | 1233339-22-4 |
Chemical Name: | 1H-Indole, 4-[4-[(3R)-3-methyl-4-morpholinyl]-6-[1-(methylsulfonyl)cyclopropyl]-2-pyrimidinyl]- |
Synonyms: | AZ-20; AZ 20, |
SMILES: | O=S(C1(C2=CC(N3[C@H](C)COCC3)=NC(C4=CC=CC5=C4C=CN5)=N2)CC1)(C)=O |
Formula: | C21H24N4O3S |
M.Wt: | 412.51 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM). |
In Vivo: | AZ20 (25, 50 mg/kg, p.o.) has high permeability combined with good stability to rat hepatocytes and, despite the lack of progress in achieving markedly higher solubility, has respectable bioavailability in a low dose rat PK study. AZ20 (25, 50 mg/kg, p.o.) leads to significant tumor growth inhibition in female nude mice bearing LoVo tumors[1]. |
In Vitro: | AZ20 inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC50 of 5 nM and ATR mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma tumor cells with an IC50 of 50 nM[1]. |