Daraxonrasib

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].

Product Specifications

CAS Number

[2765081-21-6]

Product Name Alternative

RMC-6236; RAS-IN-2

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

PERK; Ras

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C44H58N8O5S

Molecular Weight

811.05

Precautions

H302, H315, H319

References & Citations

[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.