Cayman TP-0903

TP-0903 is an inhibitor of the receptor tyrosine kinase Axl (IC₅₀ = 27 nM ). It 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. TP-0903 decreases the phosphorylation of Akt and Axl in GAS6-stimulated, serum-starved PSN-1 pancreatic cancer cells (EC₅₀s = 305 and 222 nM, respectively). It decreases cell viability (IC₅₀ = 6 nM) and induces cell cycle arrest at the g₂/M phase in PSN-1 cells when used at a concentration of 30 nM. TP-0903 also reduces the viability of colorectal cancer (CRC) cell lines with IC₅₀ values ranging from 4.5 to 123 nM. It exhibits 69 and 44% tumor growth inhibition in an HCT116 mouse xenograft model and a K-Ras-mutant CRC patient-derived xenograft (PDX) mouse model, respectively, when administered at a dose of 40 mg/kg.

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