TP-3654

TP-3654 is an inhibitor of Pim kinases (Kis = 5, 239, and 42 nM for Pim-1, Pim-2, and Pim-3, respectively). It inhibits 19 additional kinases, including PI3Kalpha, PI3Kgamma, and PI3Kdelta, with IC50 values of less than 300 nM. TP-3654 inhibits phosphorylation of Bad in HEK293 cells overexpressing Bad and Pim-1 (EC50 = 67 nM), as well as in UM-UC-3 cells. It reduces tumor growth in UM-UC-3 bladder carcinoma and PC3 prostate adenocarcinoma mouse xenograft models when administered at a dose of 200 mg/kg.Formal Name: trans-alpha,alpha-dimethyl-4-[[3-[3-(trifluoromethyl)phenyl]imidazo[1,2-b]pyridazin-6-yl]amino]-cyclohexanemethanol. CAS Number: 1361951-15-6. Molecular Formula: C22H25F3N4O. Formula Weight: 418.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMSO: 16 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 10 mg/ml. lambdamax: 217, 274, 342 nm. SMILES: CC(C)(O)[C@H]1CC[C@H](NC2=NN3C(C=C2)=NC=C3C4=CC=CC(C(F)(F)F)=C4)CC1. InChi Code: InChI=1S/C22H25F3N4O/c1-21(2,30)15-6-8-17(9-7-15)27-19-10-11-20-26-13-18(29(20)28-19)14-4-3-5-16(12-14)22(23,24)25/h3-5,10-13,15,17,30H,6-9H2,1-2H3,(H,27,28)/t15-,17-. InChi Key: XRNVABDYQLHODA-JCNLHEQBSA-N.