ARS-1620( ARS1620 )

Catalog No. M12591 CAS No. 1698055-85-4

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

ARS-1620
Note

Research use only, not for human use.
Brief Description

ARS-1620 is a potent, specific and covalent KRAS G12C inhibitor.
Description

ARS-1620 is a potent, specific and covalent KRAS G12C inhibitor with an observed rate of 1,100±200 M-1S-1, shows >10-fold improved potency over the initial ARS-853; inhibits RAS signaling with IC50 of 120 nM, exhibits a half maximal G12C target engagement (TE50) at 0.3 uM and near complete engagement at 3.0 uM across a panel of cell lines harboring the mutant allele; achieves rapid and sustained in vivo target occupancy to induce tumor regression, and is a novel generation of KRASG12C-specific inhibitor with promising therapeutic potential.
Synonyms

ARS1620
Pathway

MAPK/ERK Signaling
Target

Ras
Recptor

Ras
Research Area

Cancer
Indication

——

CAS Number

1698055-85-4
Formula Weight

430.84
Molecular Formula

C21H17ClF2N4O2
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 53 mg/mL 123.02 mM
SMILES

C=CC(N1CCN(C2=C3C=C(Cl)[C@@]([C@@]4=C(O)C=CC=C4F)=C(F)C3=NC=N2)CC1)=O
Chemical Name

(S)-1-(4-(6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)quinazolin-4-yl)piperazin-1-yl)prop-2-en-1-one

1. Janes MR, et al. Cell. 2018 Jan 25;172(3):578-589.e17.

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