BDP9066

BDP9066 is an inhibitor of Cdc42-binding kinase alpha (MRCKalpha) and MRCKbeta (Kis = 0.0136 and 0.0233 nM, respectively). It is selective for MRCKalpha and MRCKbeta over Rho-associated kinase 1 (ROCK1) and ROCK2 (Kis = 18.4 and 5.38 nM, respectively) and a panel of 115 additional kinases at 1 µM. BDP9066 has antiproliferative activity against a panel of 757 cancer cell lines (EC50s = 50 = 64 nM) and inhibits the motility of the same cells. BDP9066 (25 µg/animal) decreases average papilloma volume in a mouse two-stage model of skin carcinogenesis initiated by 7,12-dimethylbenz[a]anthracene (DMBA, Cay-30383) and promoted by phorbol 12-myristate 13-acetate (TPA, Cay-10008014).Formal Name: (6S)-8-[3-(4-pyrimidinyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1,8-diazaspiro[5.5]undecane. CAS Number: 2226507-04-4. Molecular Formula: C20H24N6. Formula Weight: 348.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, DMSO: Sparingly soluble: 1-10 mg/ml, Water: Slightly soluble: 0.1-1 mg/ml. SMILES: C1(C(C2=NC=NC=C2)=CN3)=C3N=CC=C1N4C[C@@]5(NCCCC5)CCC4. InChi Code: InChI=1S/C20H24N6/c1-2-8-25-20(6-1)7-3-11-26(13-20)17-5-10-22-19-18(17)15(12-23-19)16-4-9-21-14-24-16/h4-5,9-10,12,14,25H,1-3,6-8,11,13H2,(H,22,23)/t20-/m0/s1. InChi Key: UELSMLDRSQFVHG-FQEVSTJZSA-N.