购物车
- 全部删除
- 您的购物车当前为空
NMS-E973 是一种有效且选择性的 Hsp90 抑制剂,与 Hsp90 结合的 DC50小于 10 nM。它能够穿越血脑屏障,具有抗肿瘤效果。
为众多的药物研发团队赋能,
让新药发现更简单!
NMS-E973 是一种有效且选择性的 Hsp90 抑制剂,与 Hsp90 结合的 DC50小于 10 nM。它能够穿越血脑屏障,具有抗肿瘤效果。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 196 | 现货 | |
5 mg | ¥ 443 | 现货 | |
10 mg | ¥ 738 | 现货 | |
25 mg | ¥ 1,550 | 现货 | |
50 mg | ¥ 2,270 | 现货 | |
100 mg | ¥ 3,250 | 现货 | |
200 mg | ¥ 4,570 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 493 | 现货 |
产品描述 | NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. |
靶点活性 | HSP90:<10 nM(DC50) |
体外活性 | NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein, such as Flt3, B-Raf, AKT, which further blocks tumor-related pathways, such as the Raf/MAPK, PI3K/AKT, and JAK/STAT pathways. [1] |
体内活性 | NMS-E973 (10 mg/kg i.v.) shows a favorable pharmacokinetic profile with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 (60 mg/kg i.v.) shows high antitumor efficacy in all the models tested, including A375 and A2780 xenografts. In addition, NMS-E973 (10 mg/kg i.v.) together with B-Raf inhibitor PLX-4720 at 100 mg/kg produces a synergic anti-tumor effect. [1] In a mouse model of human ovarian cancer, NMS-E973 produces the antitumor activity by inhibition of Hsp90. [2] |
激酶实验 | Hsp90 binding assays: For competition experiments, a protein concentration of 5 nM for Hsp90 and of 200 nM for Trap1 are mixed with 0.5 nmol/L probe (final concentrations). After incubation, the dimethyl sulfoxide (DMSO) compound solution is added to the mixture. The plate is incubated for 18 hours at room temperature and then the fluorescence polarization signal was measured. Data are fitted with the program Dynafit version 3.28.039 or SigmaPlot (SSI) using the mathematical equation for competitive binding of 2 ligands to the receptor. |
分子量 | 454.43 |
分子式 | C22H22N4O7 |
CAS No. | 1253584-84-7 |
Smiles | CN1CCC(CC1)NC(=O)c1cc(on1)-c1c(O)cc(O)cc1Oc1ccc(cc1)[N+]([O-])=O |
密度 | 1.50 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 83 mg/mL (182.6 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容