ARS-853 (ARS853)

For research use only.

Catalog No.S8156

1 publication

ARS-853 (ARS853) Chemical Structure

Molecular Weight(MW): 432.94

ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.

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Selleck's ARS-853 (ARS853) has been cited by 1 publication

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Biological Activity

Description ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
K-Ras(G12C) [2]
(in H358 cells)
2.5 μM
In vitro

ARS-853 treatment of KRASG12C cells led to a dose-dependent and nearly complete inhibition of CRAF-RBD (RBD)-mediated pulldown of KRAS from lysates, with an IC50 of approximately 1 μmol/L. Treatment of H358 cells by ARS-853 resulted in a significant loss of KRAS–CRAF interactions. Consistent with an inactive state of KRASG12C once bound to ARS-853, downstream signaling through both MAPK (including pMEK, pERK, and pRSK) and PI3K signaling (pAKT) pathways was inhibited by ARS-853 in H358 and other KRASG12C cell lines. The inhibition of RAF-RBD pulldown and KRAS downstream signaling was sustained over a period of 72 hours, accompanied by G1 cell-cycle arrest, loss of Cyclin D1 and Rb expression, and an increase in the cell-cycle inhibitor p27 KIP1. In addition, hallmarks of apoptosis, including cleaved PARP and increases in sub-diploid DNA, were observed in H358 cells following treatment with ARS-853. No effects on RAF-RBD binding or downstream signaling were observed in A549 cells (KRASG12S), and the inhibitory effects of ARS-853 in H358 cells could be rescued by ectopic expression of KRASG12V. KRASG12C is the most potent covalent target of ARS-853 across more than 2,700 cellular proteins and consistently find that this compound exerts no effects on cellular signaling or growth in non-KRASG12C cells at concentrations up to 10-fold higher than its KRASG12C potency. ARS-853 reacts only with the inactive (GDP-bound), but the not the active (GTP-bound), state of KRAS[1]. ARS853 reduced KRAS-GTP levels and ERK phosphorylation in human embryonic kidney 293 (HEK293) or H358 cells engineered to express KRASG12C but not in those expressing KRASG12C/A59G. ARS853 traps KRASG12C in a GDP-bound conformation by lowering its affinity for nucleotide exchange factors[2].


Cell Research:


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  • Cell lines: H358 (G12C) cells
  • Concentrations: 0.05, 0.1, 0.5, 1, 5, 10, 50 μM
  • Incubation Time: 5 h
  • Method:

    KRASG12C mutant cells (H358) were treated with ARS853 for 5 hours. The effect on the level of active, or GTP-bound, KRAS was determined by a RAS-binding domain pull-down (RBD:PD) assay and immunoblotting with a KRAS-specific antibody. 

    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL warmed (198.64 mM)
Ethanol 1 mg/mL warmed (2.3 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 432.94


CAS No. 1629268-00-3
Storage powder
in solvent
Synonyms N/A
Smiles CC1(CC1)C2=C(Cl)C=C(O)C(=C2)NCC(=O)N3CCN(CC3)C4CN(C4)C(=O)C=C

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID