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ARS-853

Chemical Structure : ARS-853

CAS No.: 1629268-00-3

ARS-853 (ARS853;ARS 853)

Catalog No.: PC-45673Not For Human Use, Lab Use Only.

ARS-853 (ARS853) is a mutant-specific, covalent inhibitor of KRAS G12C with IC50 of 2.5 uM.

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Biological Activity

ARS-853 (ARS853) is a mutant-specific, covalent inhibitor of KRAS G12C with IC50 of 2.5 uM.
ARS-853 engages KRASG12C in biochemical assay with a rate constant of 76 M-1s-1, > 600-fold improvement compared with Compound 12 (Ostrem JM, Nature 2013;503:548–51.).
ARS-853 inhibits growth of H358 cells.
ARS-853 is the first direct KRAS inhibitor shown to selectively inhibit KRAS in cells with potency in the range of a drug candidate.

Physicochemical Properties

M.Wt 432.9437
Formula C22H29ClN4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 71 mg/mL

Chemical Name/SMILES

2-Propen-1-one, 1-[3-[4-[2-[[4-chloro-2-hydroxy-5-(1-methylcyclopropyl)phenyl]amino]acetyl]-1-piperazinyl]-1-azetidinyl]-

References

1. Patricelli MP, et al. Cancer Discov. 2016 Mar;6(3):316-29.

2. Lito P, et al. Science. 2016 Feb 5;351(6273):604-8.

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