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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
A939572
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1032229-33-6
- 规格：
10mg/50mg/25mg/2mg/5mg
| 规格： | 10mg | 产品价格： | ￥1340.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥5190.0 |
| 规格： | 25mg | 产品价格： | ￥2600.0 |
| 规格： | 2mg | 产品价格： | ￥650.0 |
| 规格： | 5mg | 产品价格： | ￥980.0 |
| 基本信息 | |
| CAS | No.1032229-33-6 |
| 英文名称 | A939572 |
| 分子式 | C20H22ClN3O3 |
| 分子量 | 387.86 |
| 溶解性 | Soluble in DMSO ≥3mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD10698997 |
| SMILES | CNC(=O)C1=CC(=CC=C1)NC(=O)N2CCC(CC2)OC3=CC=CC=C3Cl |
| InChIKey | DPYTYQFYDLYWHZ-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H22ClN3O3/c1-22-19(25)14-5-4-6-15(13-14)23-20(26)24-11-9-16(10-12-24)27-18-8-3-2-7-17(18)21/h2-8，13，16H，9-12H2，1H3，(H，22，25)(H，23，26) |
| PubChem CID | 24905400 |
| 靶点 | Stearoyl-CoA Desaturase (SCD1) |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | A939572 是一种有效的硬脂酰 CoA 去饱和酶 1 SCD1 抑制剂。 |
| 生物活性 | A939572 is a potent， and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1， respectively.[1] |
| IC50 | IC50: <4 nM (mSCD1)， 37 nM (hSCD1)[1] |
| In Vitro | A939572 exhibits robust in vivo activity with dose-dependent desaturation index lowering effects[1]. A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1， A498， Caki2， and ACHN at day 5 (IC50s of 65 nM， 50 nM， 65 nM， and 6 nM， respectively). In A939572 (SCDi) treated Caki1 and A498 cells， all five ER stress related genes are expressed at significantly increased levels compared to DMSO+BSA control， and this elevated expression can be blocked with the addition of OA-BSA[2]. |
| 细胞实验 | Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts are treated with A939572 (30mg/kg， p.o.) and Tem individually or in combination over the course of four weeks， and tumor volume (mm3) is recorded. A939572 and Tem monotherapy generate similar growth responses with approximately 20-30% reductions in tumor volume (vs. placebo control) being observed upon study completion， with values reaching statistical significance only within the last week of treatment. The combination group yields over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment[2]. |
| 细胞实验 | Cells are plated (0.5 or 1×105/well) in 24-well plates in triplicate. Cells are counted using a Coulter Particle Counter. Oleic acid-albumin is added to media at 5μMol. A939572 stocks are prepared in DMSO. Temsirolimus dosing is performed. Soft agar cultures are prepared by diluting 2× growth medium 1:1 in 1.5% Seaplaque?GTG? agarose， with 500 cells/plate in 60mm culture dishes. Colonies are stained with Giemsa and counted after 3wks[2]. |
| 动物实验 | A498 cells are subcutaneously implanted in athymic nu/nu mice at 1×106 cells/mouse in 50% Matrigel. Tumors reach ~50 mm3 prior to 4 wk treatment. A939572 is re-suspended in strawberry flavored Kool-Aid? in sterilized H2O (0.2 g/mL) vehicle at 30 mg/kg in a 50 μL dose. Mice are orally fed by using a syringe to administer the 50 μL dose twice daily/mouse. This modified method is found to be effective and less stressful on the mice. Temsirolimus is solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10 mg/kg in a 50 μL dose once every 72 hrs/mouse. Tumor volumes are calculated using the formula 0.5236 (L*W*H) and body weight are measured every 3 days.[2] |
| 数据来源文献 | [1]. Xin Z， et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302. [2]. von Roemeling CA， et al. Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368-80. |
| 单位 | 瓶 |
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