RM-041
RM-041 is a selective, orally active KRASG13C (ON) inhibitor that forms a covalent complex with KRASG13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRASG13C mutant cancer cells. RM-041 induces regression of KRASG13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer.
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- CAS No.: 2953276-07-6
- 화학식: C54H72F3N9O8
- 분자량:1032.20
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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KRAS G13C |
Compared with KRASG12C, KRASG13C exhibits a higher spontaneous nucleotide exchange rate, which reduces its dependence on guanine nucleotide exchange factor (GEF) reloading and its sensitivity to upstream inhibitors such as SHP2 and SOS1. Therefore, therapies targeting KRASG13C mutant tumors need to directly inhibit KRASG13C. In addition, KRASG13C shows unique sensitivity to specific GTPase-activating proteins (GAP), including NF1[1].
Preclinical Combination Therapy Strategy:
RM-041 is used to specifically inhibit mutant KRASG13C, while combined with targeted inhibition of key upstream nodes such as SHP2 to attenuate the synergistic effects mediated by wild-type RAS signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2953276-07-6
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분자량 1032.20
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화학식 C54H72F3N9O8
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SMILES
O=C(N1COC2(C1C)CCN(CC2)C(N([C@H](C(C)C)C(N[C@H]3C(N4N[C@@H](CCC4)C(OCC(C)(CC5=[C@@]([C@@]6=C([C@H](C)OC)N=CC=C6)N(CC(F)(F)F)C7=CC=C(C8=CCCN(C3)C8)C=C57)C)=O)=O)=O)C)=O)C=C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)