1263373-43-8
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
Molecular Formula: C27H37ClN6O2
1263373-43-8 - Names and Identifiers
1263373-43-8 - Physico-chemical Properties
| Molecular Formula | C27H37ClN6O2 |
| Molar Mass | 513.07 |
| Storage Condition | Room Temprature |
| In vitro study | 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 andCRBN −/− 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 andCRBN −/− 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 andCRBN −/− 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. |
1263373-43-8 - Reference Information
| biological activity | NVP-2 is an effective, selective, non-neurotoxic and ATP competitive inhibitor of cyclin dependent kinase 9 (CDK9), with an IC50 value of 0.514 nM for CDK9/CycT activity and can induce apoptosis. |
| target | TargetValue CDK9/CycT (Cell-free say) 0.514 nM |
| Target | Value |
| CDK9/CycT (Cell-free assay) | 0.514 nM |
| in vitro study | 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 andCRBN −/− 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 andCRBN −/− 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 andCRBN −/− 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. |
| Cell Line: | Leukemia cell lines Wildtype andCRBN −/− MOLT4 cells Wildtype andCRBN −/− MOLT4 cells MOLT4 cells |
| Concentration: | 0.1233 µM-0.5736 µM 1 μM; 500 nM; 250 nM 250 nM 0-10 nM |
| Incubation Time: | 72 hours 6 hours 24 hours 72 hours |
| Result: | Inhibited Leukemia cell lines viabity. Degrade CDK9 sub-stoichiometrically at all concentrations. Induced cell apoptosis in cells and wash outed the compound relieved NVP-2-induced cell apoptosis. Exhibited anti-proliferative effects in MOLT4 cells. |
Last Update：2024-04-10 22:29:15
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