RMC-6236, pan-RAS inhibitor (TBI3976)

Description

Product Details

Formal Name: (1S,2S)-N-[(7S,13S)-21-ethyl-20-[2-[(1S)-1-methoxyethyl]-5-(4-methylpiperazin-1-yl)pyridin-3-yl]-17,17-dimethyl-8,14-dioxo-15-oxa-4-thia-9,21,27,28-tetrazapentacyclo[17.5.2.12,5.19,13.022,26]octacosa-1(25),2,5(28),19,22(26),23-hexaen-7-yl]-2-methylcyclopropane-1-carboxamide

Alternate Name: Daraxonrasib

Molecular Formula: C₄₄H₅₈N₈O₅S

Formula Weight: 811.1

CAS Number: 2765081-21-6

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (> 75 mg/ml)

Storage: -20°C

Stability: ≥ 2 years

Applications

pan-RAS inhibitor

Functions

Broad spectrum inhibitor of both mutant and wild-type KRAS, NRAS, and HRAS variants. It binds with high affinity to cyclophilin A (K_D = 55 nM) creating a binary complex that has high affinity for the active state of KRAS (K_D = 131 nM for G12V, 364 nM for G12D and 154 nM for wild type). Active in in vivo xenograft models of NSCLC, PDAC, colorectal cancer, gastric carcinoma, and ovarian adenocarcinoma.

Application Procedures

First dissolved in DMSO (> 75 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.

Research use only.

Additional information

Datasheet:

TBI3976_RMC-6236_datasheet

MSDS:

TBI3976_RMC-6236_MSDS

Research use only.