NVS-PAK1-1
| 中文名称 | NVS-PAK1-1 |
|---|---|
| 中文同义词 | PAK1变构抑制剂(NVS-PAK1-1);(S)-3-((2-氯-5-(2,2-二氟乙基)-8-氟-5H-二苯并[B,E][1,4]二氮杂卓-11-基)氨基)-N-异丙基吡咯烷-1-甲酰胺;化合物NVS-PAK1-1;NVS-PAK1-1,PAK1的强变构抑制剂 |
| 英文名称 | NVS-PAK1-1 |
| 英文同义词 | NVS-PAK1-1;(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide;NVS-PAK1-1;NVS-PAK11;NVS-PAK1 1;1-Pyrrolidinecarboxamide, 3-[[2-chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-yl]amino]-N-(1-methylethyl)-, (3S)-;NVS-PAK1-1 >=98% (HPLC);NVS-PAK11Chemicalbook;(S)-3-((2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-yl)amino)-N-isopropylpyrrolidine-1-carboxamide;Inhibitor,p21 activated kinases,NVS PAK1 1,inhibit,PAK,NVS-PAK-1-1,NVSPAK11 |
| CAS号 | 1783816-74-9 |
| 分子式 | C23H25ClF3N5O |
| 分子量 | 479.93 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;API |
| Mol文件 | 1783816-74-9.mol |
| 结构式 |  |
NVS-PAK1-1 性质
| 沸点 | 697.8±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.42±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMF：50mg/mL； DMF:PBS (pH 7.2) (1:1)：0.5 mg/mL； DMSO：50mg/mL；乙醇：20mg/mL |
| 酸度系数(pKa) | 14.02±0.40(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
IC50: 5 nM (PAK1)
NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 K d of 7 nM and a PAK2 K d of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved.
NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t 1/2 in RLM 3.5 min).
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-100519 | NVS-PAK1-1 | 1 mg | 457元 | |
| 2024/04/30 | HY-100519 | (S)-3-((2-氯-5-(2,2-二氟乙基)-8-氟-5H-二苯并[B,E][1,4]二氮杂卓-11-基)氨基)-N-异丙基吡咯烷-1-甲酰胺 NVS-PAK1-1 | 1783816-74-9 | 10mM * 1mLin DMSO | 1161元 |