UNC569

UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively). It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 µM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide (Cay-12092) and methotrexate (Cay-13960). In vivo, UNC569 (4 µM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells.Formal Name: 1-[(trans-4-aminocyclohexyl)methyl]-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine. CAS Number: 1350547-65-7. Molecular Formula: C22H29FN6. Formula Weight: 396.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2.5 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 0.2 mg/ml, Ethanol: 2 mg/ml. lambdamax: 246, 308 nm. SMILES: CCCCNC1=NC=C2C(N(C[C@H]3CC[C@H](N)CC3)N=C2C4=CC=C(F)C=C4)=N1. InChi Code: InChI=1S/C22H29FN6/c1-2-3-12-25-22-26-13-19-20(16-6-8-17(23)9-7-16)28-29(21(19)27-22)14-15-4-10-18(24)11-5-15/h6-9,13,15,18H,2-5,10-12,14,24H2,1H3,(H,25,26,27)/t15-,18-. InChi Key: OGEBRHQLRGFBNV-RZDIXWSQSA-N.