(3R,10R,14aS) -AZD4625

(3R,10R,14aS) -AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer[1][2].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; p38 MAPK; PI3K; Ras

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; MAPK/ERK Pathway; PI3K/Akt/mTOR

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/3r-10r-14as-azd4625.html

Purity

98.00

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

C=CC(N1C[C@H]2N(C3=C4C(OCC2)=C(Cl)[C@]([C@]5=C(F)C=CC=C5O)=C(F)C4=NC=N3)C[C@H]1C)=O

Molecular Formula

C24H21ClF2N4O3

Molecular Weight

486.90

References & Citations

[1]Kettle JG, et al. Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C. J Med Chem. 2022 May 12;65 (9) :6940-6952.|[2]Chakraborty A, et al. AZD4625 is a Potent and Selective Inhibitor of KRASG12C. Mol Cancer Ther. 2022 Oct 7;21 (10) :1535-1546.