3076503-34-6
Chemical Structure
MG-002
- CAS No.: 3076503-34-6
- Formula:C27H25N3O7
- Molecular Weight:503.50
IUPAC Name: (5aR,6S,7R,8R,8aS)-5a-(4-cyanophenyl)-8,8a-dihydroxy-N,1,3-trimethoxy-N-methyl-6-phenyl-5a,7,8,8a-tetrahydro-6H-cyclopenta[4,5]furo[3,2-c]pyridine-7-carboxamide
InChIKey: WTENXFJWMGLPQX-WFINZZCUSA-N
SMILES: O[C@]12[C@](OC3=CC(OC)=NC(OC)=C32)(C4=CC=C(C=C4)C#N)[C@H](C5=CC=CC=C5)[C@H]([C@H]1O)C(NOC)=O
Biological Activity: MG-002 is an orally active eIF4A1 and eIF4A2 inhibitor with a human eIF4A1 IC50 of 43 nM. MG-002 prevents competent ribosome recruitment to mRNA, inhibits cap-dependent mRNA translation, and engages eIF4A2 via the same RNA clamping mechanism to inhibit mRNA translation. MG-002 induces G2/M cell cycle delay, induces apoptosis, suppresses synthesis of c-MYC and cyclin D1, and shows minimal overt toxicity in mice. MG-002 inhibits primary triple-negative breast cancer tumor growth, attenuates metastatic spread, and enhances anti-neoplastic activity of Doxorubicin (HY-15142A) in pre-clinical models[1].
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MG-002 | MG-002 is an orally active eIF4A1 and eIF4A2 inhibitor with a human eIF4A1 IC50 of 43 nM. MG-002 prevents competent ribosome recruitment to mRNA, inhibits cap-dependent mRNA translation, and engages eIF4A2 via the same RNA clamping mechanism to inhibit mRNA translation. MG-002 induces G2/M cell cycle delay, induces apoptosis, suppresses synthesis of c-MYC and cyclin D1, and shows minimal overt toxicity in mice. MG-002 inhibits primary triple-negative breast cancer tumor growth, attenuates metastatic spread, and enhances anti-neoplastic activity of Doxorubicin (HY-15142A) in pre-clinical models. | |||||||||||||||||||||
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Keywords
