F389-0746 | MAP4K4 inhibitor | Probechem Biochemicals

Chemical Structure : F389-0746

F389-0746 (F 389-0746)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	450.94
Formula	C24H19ClN2O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-2-(3-chlorobenzylidene)-N-(4-(methylthio)benzyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-6-carboxamide

References

1. Chao-Di Chang, et al. J Enzyme Inhib Med Chem. 2023 Dec;38(1):2166039.

F389-0746 (F 389-0746)

Biological Activity

Physicochemical Properties

References

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