化合物NVP-2
| 中文名称 | 化合物NVP-2 |
|---|---|
| 中文同义词 | 化合物NVP-2;4-[[[5'-氯-2'-[[反式-4-[[(1R)-2-甲氧基-1-甲基乙基]氨基]环己基]氨基][2,4'-联吡啶]-6-[氨基]甲基]甲基]四氢-2H-吡喃-4-甲腈;4-[[[5'-氯-2'-[[反式-4-[[(R)-1-甲氧基丙烷-2-基]氨基]环己基]氨基]-[2,4'-联吡啶]-6-基]氨基]甲基]四氢-2H-吡喃-4-甲腈;4-[[[5'-氯-2'-[[反式-4-[[(1R)-2-甲氧基-1-甲基乙基]氨基]环己基]氨基][2,4'-联吡啶]-6-[氨基]甲基]甲基]四氢-2H-吡喃-4-甲腈;4-[[[5'-氯-2'-[[反式-4-[[(1R)-2-甲氧基-1-甲基乙基]氨基]环己基]氨基][2,4'-联吡啶]-6- 基]氨基]甲基]四氢-2H-吡喃-4-腈;4-(((5'-氯-2'-(((1R,4R)-4-(((R)-1-甲氧基丙-2-基)氨基)环己基)氨基)-[2,4'-联吡啶]-6-基)氨基)甲基)四氢-2H-吡喃-4-氰基;NVP 2,CDK9抑制剂;NVP-3 |
| 英文名称 | 4-((5'-chloro-2'-((1R,4r)-4-((R)-1-methoxypropan-2-ylamino)cyclohexylamino)-2,4'-bipyridin-6-ylamino)methyl)tetrahydro-2H-pyran-4-carbonitrile |
| 英文同义词 | 4-((5'-chloro-2'-((1R,4r)-4-((R)-1-methoxypropan-2-ylamino)cyclohexylamino)-2,4'-bipyridin-6-ylamino)methyl)tetrahydro-2H-pyran-4-carbonitrile;NVP-2;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-;inhibit,Apoptosis,Cyclin dependent kinase,CDK,NVP-2,Inhibitor,CRBN,CDK9,Leukemia,NVP 2,NVP2;4-[[[5’-Chloro-2’-[[trans-4-[[(R)-1-methoxypropan-2-yl]amino]cyclohexyl]amino]-[2,4’-bipyridin]-6-yl]amino]methyl]tetrahydro-2H-pyran-4-carbonitrile;4-((5'-chloro-2'-((1R,4r)-4-((R)-1-methoxypropan-2-ylami)cyclohexylami)-2,4'-bipyridin-6-ylami)methyl)tetrahydro-2H-pyran-4-carbonitrile;4-((5'-chloro-2'-((1R,4r)-4-((R)-1-methoxypropan-2-ylamino)cyclohexylamino)-2,4'-bipyridin-6-ylamino)methyl)tetrahydro-2H-pyran-4-carbonitrile |
| CAS号 | 1263373-43-8 |
| 分子式 | C27H37ClN6O2 |
| 分子量 | 513.07 |
| EINECS号 | |
| 相关类别 | 抑制剂 |
| Mol文件 | 1263373-43-8.mol |
| 结构式 |  |
化合物NVP-2 性质
| 沸点 | 704.5±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.23±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 可溶于乙醇 |
| 形态 | 固体 |
| 酸度系数(pKa) | 9.14±0.40(Predicted) |
| 颜色 | 白色至黄色 |
| 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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-12214A | NVP-2 | 1 mg | 600元 | |
| 2024/08/19 | HY-12214A | 化合物NVP-2 NVP-2 | 1263373-43-8 | 5mg | 1500元 |