Description
An inhibitor of Axl (IC50 = 27 nM ); exhibits greater than 50% inhibition of 11 kinases, including MER, TYRO3, JAK2, ALK, and Abl1, in a panel of 75 kinases at 200 nM, with IC50 values of 3 and 12.4 nM for Aurora A and B, respectively; decreases the phosphorylation of Akt and Axl in GAS6-stimulated, serum-starved PSN-1 pancreatic cancer cells (EC50s = 305 and 222 nM, respectively); decreases cell viability (IC50 = 6 nM) and induces cell cycle arrest at the G2/M phase in PSN-1 cells at 30 nM; reduces the viability of CRC cell lines (IC50s = 4.5-123 nM); exhibits 69 and 44% tumor growth inhibition in an HCT116 mouse xenograft model and a K-Ras-mutant CRC PDX mouse model, respectively, at 40 mg/kg
Formal name: 2-[[5-chloro-2-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-4-pyrimidinyl]amino]-N,N-dimethyl-benzenesulfonamide
Synonyms:
Molecular weight: 516.1
CAS: 1341200-45-0
Purity: ≥98%
Formulation: A crystalline solid
