Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A939572 是口服具有活性的硬脂酰 CoA 去饱和酶 1SCD1抑制剂,对mSCD1和hSCD1的IC50分别为 <4 nM 和 37 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 349 | 现货 | ||
2 mg | ¥ 498 | 现货 | ||
5 mg | ¥ 763 | 现货 | ||
10 mg | ¥ 996 | 现货 | ||
25 mg | ¥ 2,280 | 现货 | ||
50 mg | ¥ 3,550 | 现货 | ||
100 mg | ¥ 5,130 | 现货 | ||
500 mg | ¥ 10,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 686 | 现货 |
产品描述 | A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1. |
靶点活性 | hSCD1:37 nM, mSCD1:<4 nM |
体外活性 | A939572 has been used to induce cell death of hPSCs as well as to inhibit the proliferation of human non-small cell lung carcinoma H1299 cells in vitro[1][2]. |
体内活性 | Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts were treated with A939572 and Tem individually or in combination over the course of four weeks, and tumor volume (mm3) was recorded .?A939572 and Tem monotherapy generated 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 yielded over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment.?All of the animals maintained a healthy weight throughout the course of the treatment , however those in both the A939572 and the Combo group exhibited increased blinking, and slight mucosal discharge from the eyes after the first week of treatment[3]. |
激酶实验 | Caki1 and A498 cells were transiently transfected with p5xATF6-GL3 UPR luciferase reporter and pRL-CMV-renilla luciferase plasmid using Lipofectamine2000 (Invitrogen). Cells (DMSO vs. A939572, NT vs. shSCD780) were harvested after 48hrs using Dual Luciferase assay kit per the manufacturer s protocol and luciferase activity was measured using a Veritas Luminometer; reported as relative luminescence[3]. |
动物实验 | A498 cells were subcutaneously implanted in athymic nu/nu mice at 1×10^6 cells/mouse in 50%Matrigel.?Tumors reached ~50 mm^3 prior to 4wk treatment.?A939572 was re-suspended in strawberry-flavored Kool-Aid in sterilized H2O (0.2g/mL) vehicle at 30mg/kg in a 50μl dose.?Mice were orally fed by using a syringe to administer the 50μl dose twice daily/mouse.?This modified method was found to be effective and less stressful on the mice.?Temsirolimus was solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10mg/kg in a 50μl dose once every 72hrs/mouse.?Tumor volumes were calculated using the formula and body weight were measured every 3 days[3]. |
分子量 | 387.86 |
分子式 | C20H22ClN3O3 |
CAS No. | 1032229-33-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 56 mg/mL (144.38 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5782 mL | 12.8912 mL | 25.7825 mL | 64.4562 mL |
5 mM | 0.5156 mL | 2.5782 mL | 5.1565 mL | 12.8912 mL | |
10 mM | 0.2578 mL | 1.2891 mL | 2.5782 mL | 6.4456 mL | |
20 mM | 0.1289 mL | 0.6446 mL | 1.2891 mL | 3.2228 mL | |
50 mM | 0.0516 mL | 0.2578 mL | 0.5156 mL | 1.2891 mL | |
100 mM | 0.0258 mL | 0.1289 mL | 0.2578 mL | 0.6446 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
A939572 1032229-33-6 Metabolism Dehydrogenase Stearoyl-CoA Desaturase (SCD) Inhibitor inhibit A-939572 A 939572 inhibitor