Divarasib

Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

Product Specifications

CAS Number

[2417987-45-0]

Product Name Alternative

GDC-6036

UNSPSC

12352005

Target

Ras

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/divarasib.html

Purity

99.31

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

NC1=N[C@]([C@]2=C(C=C3C(N=C(N=C3N4[C@H](CN(CC4)C(C=C)=O)C)OC[C@H]5N(CCC5)C)=C2F)Cl)=C(C(C)=C1)C(F)(F)F

Molecular Formula

C29H32ClF4N7O2

Molecular Weight

622.06

References & Citations

[1]Sushant Malhotra, et al. Fused ring compounds. WO2020097537A2.|[2]Lingyao Meng, et al. Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC-MS/MS Approach. Anal Chem. 2022 Sep 20;94 (37) :12927-12933.