CH5424802

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. CH5424802 is an ATP-competitive inhibitor of ALK (IC50 = 1.9 nM) that also inhibits F1174L, R1275Q, and L1196M mutants of ALK (IC50s = 1.0, 3.5, and 1.6 nM, respectively). It shows more than 500-fold selectivity for ALK over a panel of 24 other kinases. CH5424802 is orally available and inhibits the growth of tumors in mouse xenograft models of nonsmall cell lung cancer and anaplastic large-cell lymphoma.Formal Name: 9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile. CAS Number: 1256580-46-7. Synonyms: Alectinib, RO5424802. Molecular Formula: C30H34N4O2. Formula Weight: 482.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/mL, DMF:PBS(pH7.2) (1:2): 0.3 mg/mL. lambdamax: 232, 262, 281, 337 nm. SMILES: CCC1=CC2=C(C(C)(C)C(NC3=C4C=CC(C#N)=C3)=C4C2=O)C=C1N(CC5)CCC5N6CCOCC6. InChi Code: InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3. InChi Key: KDGFLJKFZUIJMX-UHFFFAOYSA-N.