NVS-PAK1-1
|
|
|
- CAS号:
- 1783816-74-9
- 英文名:
- NVS-PAK1-1
- 英文别名:
- NVS-PAK1-1;NVS-PAK11Chemicalbook;NVS-PAK1-1 >=98% (HPLC);NVS-PAK1-1;NVS-PAK11;NVS-PAK1 1;Inhibitor,p21 activated kinases,NVS PAK1 1,inhibit,PAK,NVS-PAK-1-1,NVSPAK11;(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide;(S)-3-((2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-yl)amino)-N-isopropylpyrrolidine-1-carboxamide;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)-
- 中文名:
- NVS-PAK1-1
- 中文别名:
- 化合物NVS-PAK1-1;PAK1变构抑制剂(NVS-PAK1-1);NVS-PAK1-1,PAK1的强变构抑制剂;(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
- CBNumber:
- CB63333615
- 分子式:
- C23H25ClF3N5O
- 分子量:
- 479.93
- MOL File:
- 1783816-74-9.mol
|
|
|
NVS-PAK1-1化学性质
-
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: 50 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 50 mg/ml; Ethanol: 20 mg/ml
-
|
-
酸度系数(pKa):
-
14.02±0.40(Predicted)
-
|
-
形态:
-
powder
-
|
-
颜色:
-
white to beige
-
|
NVS-PAK1-1性质、用途与生产工艺
NVS-PAK1-1是有效，选择性的 PAK1 变构抑制剂，IC50值为5 nM。
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).
NVS-PAK1-1
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-100519 | NVS-PAK1-1 | | 1 mg | 457元 |
| 2024/01/25 | 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 | 5mg | 1100元 |
1783816-74-9, NVS-PAK1-1 相关搜索:
- API
- 生物试剂
- 细胞生物学试剂
- NVS-PAK1-1,PAK1的强变构抑制剂
- 化合物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
- PAK1变构抑制剂(NVS-PAK1-1)
- 1783816-74-9
- Inhibitor,p21 activated kinases,NVS PAK1 1,inhibit,PAK,NVS-PAK-1-1,NVSPAK11
- (S)-3-((2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-yl)amino)-N-isopropylpyrrolidine-1-carboxamide
- NVS-PAK11Chemicalbook
- NVS-PAK1-1 >=98% (HPLC)
- 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;NVS-PAK11;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