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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:
406228-55-5
- 规格:
10 mM * 1 mL///100 mg
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A-385358
CAS No. : 406228-55-5
MCE 国际站:A-385358
产品活性:A-385358 是 Bcl-XL 的一个选择性抑制剂,对于 Bcl-XL 和 Bcl-2 的 Ki 值分别为 0.80 和 67 nM。
研究领域:Apoptosis
作用靶点:Bcl-2 Family
In Vitro: A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively, in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-XL cells for 24 hours with A-385358 results in cell killing with an EC50 of 0.47±0.05 μM (n=68). This effect is accompanied by an increase in caspase-3 activity. Consistent with the greater affinity for the Bcl-XL versus Bcl-2 hydrophobic grooves, the EC50 of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells (1.9±0.1 μM; n=55) is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-XL cells. In addition, A-385358 is more effective at stimulating cytochrome c release from mitochondria isolated from FL5.12/Bcl-XL versus Bcl-2 cells.
In Vivo: The combination of A-385358 given at 100 mg/kg/d plus the lower dose of paclitaxel produces a significant reduction in tumor growth (%T/C) compare with paclitaxel monotherapy. This combination also yields a >100% increase in time for tumors to reach 900 mm3 (%ILS) compare with vehicle control. Maximal efficacy is observed during the dosing period for A-385358, with slow but steady increase in the tumor growth after termination of treatment. The combination of A-385358 at 75 mg/kg/d plus paclitaxel at 30 mg/kg/d is also well tolerated and inhibits tumor growth rate by nearly 80%. Significant effects on tumor growth relative to paclitaxel monotherapy are observed with doses as low as 50 mg/kg/d.
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文献和实验μL 体系 2× MasterMix 25 μL 上游 Primer ( 10 μM 1-5 μL 下游 Primer ( 10 μM ) 1-5 μL 模板 lamid DNA ~ 50 ng genomic DNA ~ 1000 ng cDNA ~ 500 ng 粗提液 ~ 2 μL 灭菌蒸馏水至 50 μL PCR 扩增实例: 一、plasmid DNA 扩增 1.提取的质粒 DNA 扩增 以pUC19 质粒为模板扩增 100,250,500
DNA EXTRACTION FROM MICRODISSECTED PARAFFIN SECTIONS
diiferent blades for each part of the tumor. Overlay with 20 ul mineral oil. Close cap and seal with parafilm. DIGESTION: Incubate overnight for shaking at 120 rpm, 55 C. Day 2: Add 0.3 ul fresh conc Proteinase K (20 mg/ml stock
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