Bosutinib

Bosutinib is an inhibitor of c-Src and Abl kinases (IC50s = 1.2 and 1 nM, respectively). It also inhibits the kinases EPHB2, TrkA, TrkB, and TXK (IC50s = 8.5, 22, 27, and 40 nM, respectively) among others. Bosutinib inhibits Src-dependent cell proliferation (IC50 = 100 nM) and reverses Src-transformed fibroblasts to a non-transformed morphology when used at a concentration of 1 µM. It reduces tumor growth in unstaged and staged Src-transformed fibroblast mouse xenograft models when administered at doses of 30 or 25 mg/kg, respectively, twice per day. Bosutinib (100 mg/kg) also induces complete tumor regression in a K562 mouse xenograft model when administered once per day for five days.Formal Name: 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile. CAS Number: 380843-75-4. Synonyms: SKI 606. Molecular Formula: C26H29Cl2N5O3. Formula Weight: 530.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml, PBS (pH 7.2): 1 mg/ml. lambdamax: 269, 344 nm. SMILES: CN1CCN(CCCOC2=C(OC)C=C(C(NC3=CC(OC)=C(Cl)C=C3Cl)=C(C#N)C=N4)C4=C2)CC1. InChi Code: InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31). InChi Key: UBPYILGKFZZVDX-UHFFFAOYSA-N.