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SML4213

RMC-6236

≥98% (HPLC)

Synonym(s):

(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, Cyclopropanecarboxamide, N-[(2R,14S,18S)-1-ethyl-18,19,20,21-tetrahydro-2-[2-[(1S)-1-methoxyethyl]-5-(4-methyl-1-piperazinyl)-3-pyridinyl]-25,25-dimethyl-15,22-dioxo-17H-5,3-([4,2]-endo-thiazolopropano[1,3]-endo-pyridazinomethanoxypropano)-1H-indol-14-yl]-2-methyl-, (1S,2S)- (ACI), RAS-IN-2, RAS inhibitor 2, RMC 6236, RMC6236

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About This Item

Empirical Formula (Hill Notation):
C44H58N8O5S
CAS Number:
2765081-21-6
Molecular Weight:
811.05
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Biochem/physiol Actions

RMC-6236 is an orally active, potent RAS inhibitor that targets the active, GTP-bound wild-type (RAS-RAF complex disruption IC50 = 66/82/85 nM using NRAS/HRAS/KRAS) and mutant variants (IC50 = 28-200 nM) of canonical RAS isoforms. RMC-6236 inhibits RAS-mediated cellular signaling (pERK IC50 = 0.25-4.5 nM in 12 cancer cultures) and RAS-dependent cancer proliferation both in cultures (IC50 = 1.2 nM/HPAC and 1.4 nM/Capan-2) and in KRASG12X xenograft models in mice in vivo (10-25 mg/kg/day p.o.), including NCI-H441 (KRASG12V/WT, NSCLC), NCI-H358 (KRASG12C/WT, NSCLC) , Capan-2 (KRASG12V/WT, PDAC) and HPAC (KRASG12D/WT, PDAC).

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Codes

H302,H315

Hazard Classifications

Acute Tox. 4 Oral - Skin Irrit. 2

Storage Class

11 - Combustible Solids

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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