1783816-74-9
1783816-74-9 結(jié)構(gòu)式
基本信息
NVS-PAK1-1 >=98% (HPLC)
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
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)-
物理化學(xué)性質(zhì)
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2025/12/22 | HY-100519 | NVS-PAK1-1 | 1783816-74-9 | 1 mg | 454元 |
| 2025/12/22 | HY-100519 | (S)-3-((2-氯-5-(2,2-二氟乙基)-8-氟-5H-二苯并[B,E][1,4]二氮雜卓-11-基)氨基)-N-異丙基吡咯烷-1-甲酰胺 NVS-PAK1-1 | 1783816-74-9 | 5mg | 1100元 |
| 2025/12/22 | HY-100519 | (S)-3-((2-氯-5-(2,2-二氟乙基)-8-氟-5H-二苯并[B,E][1,4]二氮雜卓-11-基)氨基)-N-異丙基吡咯烷-1-甲酰胺 NVS-PAK1-1 | 1783816-74-9 | 10mM * 1mLin DMSO | 1161元 |
常見問題列表
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).