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ARS-853 (ARS853)

Ras抑制剂

规格或纯度: 95%

CAS编号: 1629268-00-3
分子式: C₂₂H₂₉ClN₄O₃
分子量: 432.94
PubChem编号: 86279165

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货号 (SKU)	包装规格	是否现货	价格	数量
A413921-1mg	1mg	现货
A413921-5mg	5mg	现货
A413921-10mg	10mg	现货
A413921-25mg	25mg	现货
A413921-50mg	50mg	期货

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基本描述

英文别名	2-Propen-1-one,1-[3-[4-[2-[[4-chloro-2-hydroxy-5-(1-methylcyclopropyl)phenyl]amino]acetyl]-1-piperazinyl]-1-azetidinyl]-
规格或纯度	95%
英文名称	ARS-853 (ARS853)
生化机理	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. ARS-853 also induces apoptosis.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Information ARS-853 (ARS853) 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. ARS-853 also induces apoptosis . Targets K-Ras(G12C) (in H358 cells) 2.5 μM In vitro ARS-853 treatment of KRAS^G12C 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 KRAS^G12C 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 KRAS^G12C 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 KRAS^G12V. KRAS^G12C 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-KRAS^G12C cells at concentrations up to 10-fold higher than its KRAS^G12C potency. ARS-853 reacts only with the inactive (GDP-bound), but the not the active (GTP-bound), state of KRAS. ARS853 reduced KRAS-GTP levels and ERK phosphorylation in human embryonic kidney 293 (HEK293) or H358 cells engineered to express KRAS^G12C but not in those expressing KRAS^G12C/A59G. ARS853 traps KRAS^G12C in a GDP-bound conformation by lowering its affinity for nucleotide exchange factors. Cell Research(from reference) Cell lines：H358 (G12C) cells Concentrations：0.05, 0.1, 0.5, 1, 5, 10, 50 μM Incubation Time：5 h

名称和标识符

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
InChi Key	IPFOCHMOYUMURK-UHFFFAOYSA-N
Canonical SMILES	CC1(CC1)C2=CC(=C(C=C2Cl)O)NCC(=O)N3CCN(CC3)C4CN(C4)C(=O)C=C
Isomeric SMILES	CC1(CC1)C2=CC(=C(C=C2Cl)O)NCC(=O)N3CCN(CC3)C4CN(C4)C(=O)C=C
PubChem CID	86279165
分子量	432.94

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 86 mg/mL warmed with 50ºC Water: bath (198.64 mM); Ethanol: 7 mg/mL warmed with 50ºC Water: bath (16.16 mM); Water: Insoluble;

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