Bosutinib-d8

Bosutinib-d8 is intended for use as an internal standard for the quantification of bosutinib (Cay-12030) by GC- or LC-MS. 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-methylpiperazin-1-yl-2,2,3,3,5,5,6,6-d8)propoxy)quinoline-3-carbonitrile. CAS Number: 2733145-45-2. Molecular Formula: C26H21Cl2D8N5O3. Formula Weight: 538.5. Purity: >99% deuterated forms (d1-d8). Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly Soluble, Methanol: Slightly Soluble. SMILES: CN1C([2H])([2H])C([2H])([2H])N(CCCOC2=C(OC)C=C(C(NC3=CC(OC)=C(Cl)C=C3Cl)=C(C#N)C=N4)C4=C2)C([2H])([2H])C1([2H])[2H]. 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)/i6D2,7D2,8D2,9D2. InChi Key: UBPYILGKFZZVDX-COMRDEPKSA-N.