RMC-6236

Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors[1][2][3].

2765081-21-6

RMC-6236; RAS-IN-2

12352005

H302, H315, H319

PERK; Ras

Reference compound

Cell Cycle/DNA Damage; GPCR/G Protein; MAPK/ERK Pathway

Cancer-Kinase/protease

Cancer

https://www.medchemexpress.com/rmc-6236.html

99.88

DMSO : 100 mg/mL (ultrasonic)

CC(COC([C@H]1NN(C([C@H](CC2=NC3=CS2)NC([C@H]4C[C@@H]4C)=O)=O)CCC1)=O)(C)CC5=[C@@](N(CC)C6=C5C=C3C=C6)[C@@]7=C([C@H](C)OC)N=CC(N8CCN(C)CC8)=C7

C44H58N8O5S

811.05

H302, H315, H319

[1]Jiang J, et al. Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers. Cancer Discov. 2024 Jun 3;14 (6) :994-1017.|[2]Patel H V, et al. The farnesyl transferase inhibitor KO-2806 re-sensitizes relapsing tumors to RAS inhibition. BioRxiv, 2024: 2024.12. 20.629824. |[3]Long SA, et al. Evaluation of KRAS inhibitor-directed therapies for pancreatic cancer treatment. Front Oncol. 2024 May 10;14:1402128.

Blue Ice

-20°C, 3 years (Powder)

http://file.medchemexpress.com/batch_PDF/HY-148439/Daraxonrasib-SDS-MedChemExpress.pdf

Reference compound1

Phase 3

K-Ras