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Description
RMC-6236 is a first-in-class, potent, oral RAS-selective tri-complex, RAS(MULTI)(ON) inhibitor with an attractive preclinical profile and is designed to treat cancers caused by multiple RAS variants for which no targeted treatment is currently available. Upon oral administration, RAS inhibitor RMC-6236 binds to an intracellular chaperone protein, cyclophilin A (CypA). The resulting inhibitory binary complex binds to active, GTP-bound RAS to form a tri-complex. This tri-complex inhibits RAS-dependent signaling and inhibits the proliferation of tumor cells in which RAS is overexpressed and/or mutated. RAS plays an important role in cell signaling, division and differentiation. Mutations of RAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.
Technical Data
Product Name: RMC-6236
Chemical Formula: C44H58N8O5S
Molecular Weight: 811.06
CAS#: 2765081-21-6
Appearance: Solid powder
Purity: > 99% by HPLC
Solubility: Soluble in DMSO
Storage: Room temperature for months, or -20ºC for 3 years
Targets: RAS(ON); RAS(MULTI)(ON)
Synonym: RMC-6236; RMC6236; RMC 6236, KRAS, RAS
Chemical Name/IUPAC:(1S,2S)-N-((63S,4S,Z)-11-ethyl-12-(2-((S)-1-methoxyethyl)-5-(4-methylpiperazin-1-yl)pyridin-3-yl)-10,10-dimethyl-5,7-dioxo-61,62,63,64,65,66-hexahydro-11H-8-oxa-2(4,2)-thiazola-1(5,3)-indola-6(1,3)-pyridazinacycloundecaphane-4-yl)-2-methylcyclopropane-1-carboxamide
SMILES Code: CC(COC([C@H][C@H][C@H]4C[C@@H]4C)=O)=O)CCC1)=O)(C)CC5=[C@@][C@@]7=C([C@H](C)OC)N=CC(N8CCN(C)CC8)=C7
Synonym: RMC-6236; RMC6236; RMC 6236, KRAS, RAS
Chemical Name/IUPAC:(1S,2S)-N-((63S,4S,Z)-11-ethyl-12-(2-((S)-1-methoxyethyl)-5-(4-methylpiperazin-1-yl)pyridin-3-yl)-10,10-dimethyl-5,7-dioxo-61,62,63,64,65,66-hexahydro-11H-8-oxa-2(4,2)-thiazola-1(5,3)-indola-6(1,3)-pyridazinacycloundecaphane-4-yl)-2-methylcyclopropane-1-carboxamide
SMILES Code: CC(COC([C@H][C@H][C@H]4C[C@@H]4C)=O)=O)CCC1)=O)(C)CC5=[C@@][C@@]7=C([C@H](C)OC)N=CC(N8CCN(C)CC8)=C7
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