RM-046 

RM-046 is an orally active, selective ternary complex inhibitor of KRAS^Q61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRAS^Q61H 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 KRAS^Q61H mutant cancers^[1].

Oral administration of RM-041 enables profound, sustained inhibition of RAS pathway activity in human KRAS^Q61H xenograft tumor models (including NSCLC and PDAC), and induces in vivo tumor regression at tolerated doses^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1137.33

C₆₂H₇₉F₃N₈O₉

3058972-05-4

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yang Y C, Thompson S, Montgomery D, et al. RM-046, a first-in-class, mutant-selective, and oral KRASQ61H (ON) inhibitor that drives tumor regression in preclinical models and validates KRASQ61H as a therapeutic target[J]. Cancer Research, 2023, 83(7_Supplement): 1598-1598.