3058972-05-4
Chemical Structure
RM-046
- CAS. Nr.: 3058972-05-4
- Formula:C62H79F3N8O9
- Molecular Weight:1137.33
InChIKey: PQLCJKAFQBWNID-TWBKLVLDSA-N
SMILES: O=C([C@H](C(C)C)N1C)N[C@H](C(N2CCC[C@@H]3N2)=O)CC4=CC(C5=CC6=C(C=C5)N(CC(F)(F)F)[C@]([C@]7=C([C@H](C)OC)N=CC(C8CCN(C9CC9)CC8)=C7)=C6CC(C)(C)COC3=O)=CC(OC[C@@H](N(C(C%10(C)COC%10)=O)CC%11)[C@@H]%11C1=O)=C4
Biological Activity: RM-046 is an orally active, selective ternary complex inhibitor of KRASQ61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRASQ61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRASQ61H mutant cancers[1].
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RM-046 | RM-046 is an orally active, selective ternary complex inhibitor of KRASQ61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRASQ61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRASQ61H mutant cancers. | |||||||||||||||||||||
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