ARS-853

SKU: orb1299841

Description

ARS-853 is a small molecule inhibitor targeting the oncogenic mutant K-RASG12C (IC50: 2.5 µM). It covalently binds to the GDP-bound form, trapping it in an inactive state to inhibit proliferation in cancer cell lines. This tool compound is used in vitro to study RAS-driven tumor biology and signaling pathways.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1629268-00-3
• MW: 432.94
• Purity: 98.40% (May vary between batches)
• Formula: C₂₂H₂₉ClN₄O₃
• SMILES: CC1(CC1)c1cc(NCC(=O)N2CCN(CC2)C2CN(C2)C(=O)C=C)c(O)cc1Cl
• Target: Apoptosis,Raf,Ras
• Solubility: DMSO:5.5 mg/mL (12.7 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.31 mM)

Bioactivity

• Target IC50:
  KRas (G12C):2.5 μM
• In Vitro:
  ARS-853 decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 μM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, ARS 853, ARS853, ARS-853, cancer, inhibit, KRAS, K-Ras(G12C), mutant, inactive, G12C, Inhibitor, state, Ras, selective,covalent

Compound Identifiers

PubChem CID

86279165