(S)-Crizotinib

(S)-Crizotinib is an inhibitor of muT homolog 1 (MTH1, IC50 = 72 nM). It is selective for MTH1 over a panel of 456 kinases at 1 µM. (S)-Crizotinib (30 µM) induces oxidative DNA damage and apoptosis in SGC-7901 and BGC-823 human gastric cancer cells. It inhibits proliferation in a panel of 14 cancer cell lines expressing wild-type or various mutant forms of K-Ras and p53 (IC50s = 0.52-7.4 µM). (S)-Crizotinib (25 mg/kg, s.c.) reduces tumor growth in an SW480 mouse xenograft model.Formal Name: 3-[(1S)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine. CAS Number: 1374356-45-2. Molecular Formula: C21H22Cl2FN5O. Formula Weight: 450.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 0.5 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 270 nm. SMILES: FC1=CC=C(Cl)C([C@H](C)OC2=CC(C3=CN(C4CCNCC4)N=C3)=CN=C2N)=C1Cl. InChi Code: InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m0/s1. InChi Key: KTEIFNKAUNYNJU-LBPRGKRZSA-N.