RMC-6236 | pan-RAS inhibitor

CAS:
 2765081-21-6
Catalog Number:
 10-3976

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RMC-6236 (2765081-21-6) is broad spectrum inhibitor of both mutant and wild-type KRAS, NRAS, and HRAS variants.1,2 It binds with high affinity to cyclophilin A (KD = 55 nM) creating a binary complex that has high affinity for the active state of KRAS (KD = 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.2

References/Citations:

  1. Holderfield et al. (2024), Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy; Nature 629 919
  2. Jiang et al. (2024), Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers; Cancer Discov. 14 994
2765081-21-6, daraxonrasib, pan-RAS inhibitor, Ras inhibitor, RMC-6236, RMC-6236 supplier, RMC6236
CAS:
2765081-21-6
Catalog Number:
10-3976
Activity:
pan-RAS inhibitor
Chemical Names:
(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 Weight:
811.06
Molecular Formula:

C44H58N8O5S

Solubility:
Soluble in DMSO (>75 mg/ml)
Physical Properties:
White to off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

RMC-6236 (2765081-21-6) is broad spectrum inhibitor of both mutant and wild-type KRAS, NRAS, and HRAS variants.1,2 It binds with high affinity to cyclophilin A (KD = 55 nM) creating a binary complex that has high affinity for the active state of KRAS (KD = 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.2

References/Citations:

  1. Holderfield et al. (2024), Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy; Nature 629 919
  2. Jiang et al. (2024), Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers; Cancer Discov. 14 994

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