1263373-43-8
1263373-43-8 結(jié)構(gòu)式
基本信息
4-((5'-chloro-2'-((1R,4r)-4-((R)-1-methoxypropan-2-ylamino)cyclohexylamino)-2,4'-bipyridin-6-ylamino)methyl)tetrahydro-2H-pyran-4-carbonitrile
4-[[[5'-Chloro-2'-[[trans-4-[[(1R)-2-methoxy-1-methylethyl]amino]cyclohexyl]amino][2,4'-bipyridin]-6-yl]amino]methyl]tetrahydro-2H-pyran-4-carbonitrile
2H-Pyran-4-carbonitrile, 4-[[[5'-chloro-2'-[[trans-4-[[(1R)-2-methoxy-1-methylethyl]amino]cyclohexyl]amino][2,4'-bipyridin]-6-yl]amino]methyl]tetrahydro-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
| Target | Value |
|
CDK9/CycT
(Cell-free assay) | 0.514 nM |
NVP-2 has an anti-proliferation of leukemia cells, inhibits KOPT-K1, Jurkat, P12-ICHIKAWA, DU.528, MOLT 16, HSB-2, PF-382, SKW-3, SUP-T11, DND-41 and HPB-ALL cells with IC 50 values of 0.1688 μM, 0.1233 μM,0.5736 μM,0.1575 μM, 0.1620 μM,0.1585 μM, 0.1808 μM, 0.2589 μM, 0.0918 μM and 0.3023 μM, respectively. NVP-2 (250 nM-1 μM; 6 hours) engages CDK9 in wildtype and?CRBN ?/? MOLT4 cells at all concentrations, while CDK2 and CDK7 are unaffected. NVP-2 (0-10 nM; 72 hours) exhibits CRBN-dependent anti-proliferative and pro-apoptotic effects in MOLT4 cells, displays an IC 50 value of 9 nM. NVP-2 (250 nM; 24 hours) induces cell apoptosis in MOLT4 cells, upregulates caspase-3 and γH2A.X expression. However, while the compound washout significantly reduces the degree of apoptosis induced by NVP-2.
Cell Viability Assay
| Cell Line: | Leukemia cell lines |
| Concentration: | 0.1233 μM-0.5736 μM |
| Incubation Time: | 72 hours |
| Result: | Inhibited Leukemia cell lines viabity. |
Western Blot Analysis
| Cell Line: | Wildtype and?CRBN ?/? MOLT4 cells |
| Concentration: | 1 μM; 500 nM; 250 nM |
| Incubation Time: | 6 hours |
| Result: | Degrade CDK9 ?sub-stoichiometrically at all concentrations. |
Apoptosis Analysis
| Cell Line: | Wildtype and?CRBN ?/? MOLT4 cells |
| Concentration: | 250 nM |
| Incubation Time: | 24 hours |
| Result: | Induced cell apoptosis in cells and wash outed the compound relieved NVP-2-induced cell apoptosis. |
Cell Proliferation Assay
| Cell Line: | MOLT4 cells |
| Concentration: | 0-10 nM |
| Incubation Time: | 72 hours |
| Result: | Exhibited anti-proliferative effects in MOLT4 cells. |