Chemical Structure : F389-0746
货号: PC-20029Not For Human Use, Lab Use Only.
F389-0746 is a potent, selective and orally active MAP4K4 inhibitor with IC50 of 120.7 nM.
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F389-0746 is a potent, selective and orally active MAP4K4 inhibitor with IC50 of 120.7 nM.
F389-0746 showed a weaker activity inhibition for MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAP4K6, and MAP4K7 at 150 nM, with inhibition percentages of 0%, 8%, 7%, 17%, 44%, and 27%, respectively.
F389-0746 also showed high selectivity for MAP4K4 against a panel of 81 kinases across the kinome.
F389-0746 inhibited pancreatic cancer cells proliferation with GI50 of 6.67 μM and 8.58 μM in AsPC-1 and Panc-1 cells (72h).
F389-0746 enhanced cell apoptosis by inhibiting the JNK signalling pathway
F389-0746 (200 mg/kg, PO, QD) exhibited a comparable growth inhibitory effect to gemcitabine in xenograft mouse model subcutaneously injected with Panc-1 cells.
分子量 | 450.94 | |
分子式 | C24H19ClN2O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Chao-Di Chang, et al. J Enzyme Inhib Med Chem. 2023 Dec;38(1):2166039.
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