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- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1698055-85-4
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1990.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥849.0 |
| 规格: | 5 mg | 产品价格: | ¥2100.0 |
| 规格: | 10 mg | 产品价格: | ¥3360.0 |
| 规格: | 25 mg | 产品价格: | ¥5300.0 |
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ARS-1620
CAS No. : 1698055-85-4
MCE 国际站:ARS-1620
产品活性:ARS-1620 是一种阻转异构且有选择性的 KRASG12C 抑制剂,具有理想的药代动力学。
研究领域:GPCR/G Protein
作用靶点:Ras
In Vitro: ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics. ARS-1620 exhibits complete growth suppression of p.G12C cell lines (IC50=150 nM) with relatively benign effects on control cell lines. It is found that ARS-1620 significantly reduces expression of the gene set in p.G12C mutant cells in a time-dependent manner but not in the p.G12S mutant cells. Following a 5-day treatment period, only a minority of G12C mutant cell lines are sensitive to ARS-1620 under monolayer culture conditions, whereas in 3D-spheroid conditions, ARS-1620 elicits a robust response (p=0.0140).
In Vivo: Following a single oral dose or 5 consecutive daily doses, ARS-1620 yields average peak tumor concentrations of 1.5 μM (50 mg/kg) and 5.5 μM (200 mg/kg), respectively, that enables significant KRASG12C target occupancy (>=70% G12C-TE at 200 mg/kg) for >24 hr. In MIAPaCa2 xenografts (p.G12C), ARS-1620 significantly inhibits tumor growth (p<0.001) in a dose-dependent manner with marked regression at a dose of 200 mg/kg, given once daily. Across all tumor models employed, ARS-1620 is well tolerated over the entire 3-week treatment period. Moreover, there are no observed clinical signs or toxicity of ARS-1620 in CD-1 mice even at oral doses up to 1,000 mg/kg administered daily over a 7-day period.
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文献和实验Replication timing using transient hemimethylation
, and the transformant exhibiting the highest level of DpnI cleavage was selected (RM14-3a Meth5 strain). Protocol for methylation timing 1. Grow ~330 ml of RM14-3a expressing dam methylase (RM14-3a Meth5) to an OD660 of about 0.3 (3.85 x 106 cells/ml) at 23o C
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