MG-002 | eIF4A inhibitor | Probechem Biochemicals

Chemical Structure : MG-002

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MG-002 (MG002)

货号: PC-21688Not For Human Use, Lab Use Only.

MG-002 is a potent, second-generation, orally bioavailable eIF4A RNA helicase inhibitor, potently inhibits cap-dependent mRNA translation with IC50 of 43 nM.

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生物&药学活性

MG-002 is a potent, second-generation, orally bioavailable eIF4A RNA helicase inhibitor, potently inhibits cap-dependent mRNA translation with IC50 of 43 nM.
MG-002 stabilizes eIF4A1-RNA complexes, preferentially inhibits mRNAs with polypurine leader regions, and is a potent inhibitor of translation in vitro and in cellula.
MG-002 exhibits cell viability EC50 of 1-10 nM against TNBC lines (4T1, MDA-MB-231) and ER+/HER2+ breast cancer (BT474), which is more potent anti-neoplastic activity than eFT226.
MG-002 is primarily exerting its cytotoxic effects through eIF4A1/2 engagement.
MG-002 (0.5 mg/kg, oral) more significantly impaired mammary tumor growth compared to eFT226 in 4T1-526 tumors models, inhibited primary TNBC tumor growth through reduced cell proliferation and increased apoptosis.

物理化学性质&存储条件

分子量	503.51
分子式	C27H25N3O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(5aR,6S,7R,8R,8aS)-5a-(4-cyanophenyl)-8,8a-dihydroxy-N,1,3-trimethoxy-6-phenyl-5a,7,8,8a-tetrahydro-6H-cyclopenta[4,5]furo[3,2-c]pyridine-7-carboxamide

参考文献

1. Cencic R, et al. Proc Natl Acad Sci U S A. 2024 Jan 23;121(4):e2318093121.

MG-002 (MG002)

生物&药学活性

物理化学性质&存储条件

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MG-002 (MG002)

生物&药学活性

物理化学性质&存储条件

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