化合物NVP-2

生物活性靶点体外研究化合物NVP-2 试剂级价格

化合物NVP-2

CAS号:1263373-43-8
英文名:4-((5'-chloro-2'-((1R,4r)-4-((R)-1-methoxypropan-2-ylamino)cyclohexylamino)-2,4'-bipyridin-6-ylamino)methyl)tetrahydro-2H-pyran-4-carbonitrile
中文名:化合物NVP-2
CBNumber:CB92995844
分子式:C27H37ClN6O2
分子量:513.07
MOL File:1263373-43-8.mol

化合物NVP-2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 :Store at -20°C
溶解度 :Ethanol: soluble
形态 :A solid
酸度系数(pKa) :9.14±0.40(Predicted)
颜色 :White to yellow

化合物NVP-2性质、用途与生产工艺

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
Target Value
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.