ARS-853

• CAT Number: I002113
• CAS Number: 1629268-00-3
• Molecular Formula: C22H29ClN4O3
• Molecular Weight: 432.94
• Purity: ≥95%
• Synonyms: 1-[3-[4-[2-[[4-chloro-2-hydroxy-5-(1-methylcyclopropyl)phenyl]amino]acetyl]-1-piperazinyl]-1-azetidinyl]-2-propen-1-one
• Target: 2.5 μM (KRASG12C)[1]
• Solubility: DMSO: ≥ 71 mg/mL
• Storage: -20°C
• IUPAC Name: 1-[3-[4-[2-[4-chloro-2-hydroxy-5-(1-methylcyclopropyl)anilino]acetyl]piperazin-1-yl]azetidin-1-yl]prop-2-en-1-one
• InChI: InChI=1S/C22H29ClN4O3/c1-3-20(29)27-13-15(14-27)25-6-8-26(9-7-25)21(30)12-24-18-10-16(22(2)4-5-22)17(23)11-19(18)28/h3,10-11,15,24,28H,1,4-9,12-14H2,2H3
• InChIKey: IPFOCHMOYUMURK-UHFFFAOYSA-N
• SMILES: CC1(CC1)C2=CC(=C(C=C2Cl)O)NCC(=O)N3CCN(CC3)C4CN(C4)C(=O)C=C

ARS-853（Cat No.:I002113）is a potent and selective inhibitor that specifically targets mutant KRAS(G12C) protein, which is commonly found in various cancers. By covalently binding to the GDP-oncoprotein, ARS-853 effectively blocks the signaling pathways driven by mutant KRAS, inhibiting tumor growth. Additionally, ARS-853 can induce apoptosis, a process of programmed cell death. These combined mechanisms make ARS-853 a promising candidate for the development of targeted therapies against KRAS(G12C) mutant-driven cancers.

Reference

[1]. Lito P, et al. Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism. Science. 2016 Feb 5;351(6273):604-8.
[2]. Patricelli MP, et al. Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State. Cancer Discov. 2016 Mar;6(3):316-29.