UNC2025

UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively). It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases. UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo. Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.Formal Name: trans-4-[2-(butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-cyclohexanol. CAS Number: 1429881-91-3. Molecular Formula: C28H40N6O. Formula Weight: 476.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 10 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:9): 0.1 mg/ml. lambdamax: 222, 254, 290, 337 nm. SMILES: CCCCNC1=NC=C2C(N([C@@H]3CC[C@@H](O)CC3)C=C2C4=CC=C(CN5CCN(C)CC5)C=C4)=N1. InChi Code: InChI=1S/C28H40N6O/c1-3-4-13-29-28-30-18-25-26(20-34(27(25)31-28)23-9-11-24(35)12-10-23)22-7-5-21(6-8-22)19-33-16-14-32(2)15-17-33/h5-8,18,20,23-24,35H,3-4,9-17,19H2,1-2H3,(H,29,30,31)/t23-,24-. InChi Key: MJSHVHLADKXCML-RQNOJGIXSA-N.