ARS853

ARS853 is an inhibitor of K-RASG12C, a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells. ARS853 binds to the inactive GDP-bound state of K-RASG12C. It decreases the level of active GTP-bound K-RAS by 95% when used at a concentration of 10 µM in K-RASG12C mutant lung cancer cells. It also 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.Formal Name: 1-[3-[4-[2-[[4-chloro-2-hydroxy-5-(1-methylcyclopropyl)phenyl]amino]acetyl]-1-piperazinyl]-1-azetidinyl]-2-propen-1-one. CAS Number: 1629268-00-3. Molecular Formula: C22H29ClN4O3. Formula Weight: 432.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 50 mg/ml. lambdamax: 211, 249 nm. SMILES: CC1(CC1)C2=C(Cl)C=C(O)C(NCC(N3CCN(C4CN(C(C=C)=O)C4)CC3)=O)=C2. InChi Code: 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. InChi Key: IPFOCHMOYUMURK-UHFFFAOYSA-N.