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1263373-43-8

中文名称 化合物NVP-2
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
CAS 1263373-43-8
分子式 C27H37ClN6O2
分子量 513.07
MOL 文件 1263373-43-8.mol
更新日期 2025/05/13 16:41:03
1263373-43-8 结构式 1263373-43-8 结构式

基本信息

中文别名
化合物NVP-2
英文别名
NVP-2
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-
所属类别
生物化工:CDK 抑制剂

物理化学性质

沸点704.5±60.0 °C(Predicted)
密度1.23±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度可溶于乙醇
酸度系数(pKa)9.14±0.40(Predicted)
形态固体
颜色White to yellow

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS07
警示词警告
危险性描述H315-H319
化合物NVP-2价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-12214A化合物NVP-2
NVP-2
1263373-43-81 mg600元
2025/05/22HY-12214A化合物NVP-2
NVP-2
1263373-43-85mg1500元
2025/05/22HY-12214A化合物NVP-2
NVP-2
1263373-43-810mM * 1mLin DMSO1693元

常见问题列表

生物活性
NVP-2 是一种有效的、选择性的、非神经毒性和ATP竞争性的 cyclin dependent kinase 9 (CDK9) 的抑制剂,对CDK9/CycT活性的IC50值为0.514 nM,并可诱导细胞凋亡。
靶点
TargetValue
CDK9/CycT
(Cell-free assay)
0.514 nM
体外研究

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.
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