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- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
SB2343
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1246560-33-7
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥312.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥191.0 |
| 规格: | 5 mg | 产品价格: | ¥400.0 |
| 规格: | 10 mg | 产品价格: | ¥700.0 |
| 规格: | 25 mg | 产品价格: | ¥1250.0 |
| 规格: | 50 mg | 产品价格: | ¥1863.0 |
| 规格: | 100 mg | 产品价格: | ¥2788.0 |
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VS-5584
CAS No. : 1246560-33-7
MCE 国际站:VS-5584
产品活性:VS-5584 是一种 pan-PI3K/mTOR 激酶抑制剂,抑制 PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ 和 mTOR,IC50 分别为 16 nM, 68 nM, 42 nM, 25 nM 和 37 nM。VS-5584 同时阻断 mTORC2 和 mTORC1。
研究领域:PI3K/Akt/mTOR
In Vitro: VS-5584 is an ATP-competitive inhibitor which selectively inhibits PI3K/mTOR signaling with equivalent low nanomolar potency against all human Class I PI3K isoforms and mTOR kinase. VS-5584 (0.001, 0.01, 0.1,1,10 and 100 μM) preferentially inhibits cancer stem cells in HMLE breast cancer cells while Paclitaxel increases the percentage of cancer stem cells. VS-5584 (0.1, 1, 10, 100 and 1000 nM) reduces the number of Aldefluor-positive cancer stem cells while Paclitaxel increases the percentage of cancer stem cells. VS-5584 (10, 30, 100, 300 nM) reduces the percentage of cancer stem cells (side population) in a Hoechst dye exclusion assay. VS-5584 is a potent inhibitor of mTOR (IC50=37 nM) as well as class I PI3K isoforms (IC50: PI3Kα=16 nM; PI3Kβ=68 nM; PI3Kγ=25 nM; PI3Kδ=42 nM). All other evaluated kinases show negligible binding when tested up to 10 μM VS-5584.
In Vivo: Nude mice bearing MDA-MB-231 human breast cancer tumors are treated for 5 days with once daily oral VS-5584 (25 mg/kg). Oral treatment of tumor bearing mice with VS-5584 reduces cancer atem cells analyzed from extracted tumors. Mice are implanted with tumor fragments from a docetaxel-resistant patient-derived triple negative breast cancer. Mice are treated with VS-5584 (20 mg/kg, po, qd) or Docetaxel (20 mg/kg, i.v.). Oral VS-5584 induces tumor regression in a Docetaxel-resistant patient-derived breast cancer model. A single oral dose of VS-5584 is rapidly absorbed with a tmax of 0.9 hours and an elimination half-life of 10 hours. To determine the pharmacokinetic and pharmacodynamic relationship in tumors, PC3-tumor–bearing mice are treated with a single dose of VS-5584 and plasma and tumors are harvested after 6 hours and analyzed for concentrations of VS-5584 and effects on target efficacy biomarkers. Plasma levels of VS-5584 increase dose-dependently. For evaluation of efficacy in a Rapamycin-sensitive PC3 engraftment model, tumor-bearing mice are treated with VS-5584 for 28 days in comparison with the rapalog Everolimus. VS-5584 is well tolerated at both doses tested (11 and 25 mg/kg) with minimal weight loss (mean 4.7% on day 27). Treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively.
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文献和实验Sucrose Fractionation of Castor Bean
Materials Castor beans Gradient former Sucrose solutions in 0.01 M EDTA, pH 7.5 33%, 44%, 50%, 57%, 60% (w/v) Grinding Medium 0.4 M sucrose 0.165 M Tris-HCl buffer, pH 7.5 0.01 M KCl
*** Make sure the agar equilibrates to 55 C to 60 C before starting the assay; otherwise it will kill the cells. 3. Distribute several paper disks (Difco, #1599-33-6) into a sterile petri dish, and spot either 5 or 15 of synthetic alpha-factor (1 - 5 mg
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