ARS-1323-alkyne

ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy, providing tool support for the development of combination treatment strategies[1].

Product Specifications

CAS Number

[2436544-27-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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/ars-1323-alkyne.html

Purity

99.59

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(C=C)N1CCN(C2=NC(NCCC(N(C)CC#C)=O)=NC3=C(F)C(C4=C(O)C=CC=C4F)=C(Cl)C=C23)CC1

Molecular Formula

C28H27ClF2N6O3

Molecular Weight

569.00

Precautions

H302, H315, H319, H335

References & Citations

[1]Lou K, et al. KRASG12C inhibition produces a driver-limited state revealing collateral dependencies. Sci Signal. 2019 May 28;12 (583) . pii: eaaw9450.