(3Z,6Z)-3-[(5-tert-Butyl-1H-imidazol-4-yl)methylene]-6-(phenylmethylene)-2,5-piperazinedione Plinabulin (NPI-2358)
Plinabulin (NPI-2358)
CAS: 714272-27-2
Molecular Formula: C19H20N4O2
(3Z,6Z)-3-[(5-tert-Butyl-1H-imidazol-4-yl)methylene]-6-(phenylmethylene)-2,5-piperazinedione Plinabulin (NPI-2358) - Names and Identifiers
(3Z,6Z)-3-[(5-tert-Butyl-1H-imidazol-4-yl)methylene]-6-(phenylmethylene)-2,5-piperazinedione Plinabulin (NPI-2358) - Physico-chemical Properties
| Molecular Formula | C19H20N4O2 |
| Molar Mass | 336.39 |
| Density | 1.267 |
| Storage Condition | -20℃ |
| In vitro study | NPI-2358 binds to the colchicine binding site of tubulin, effectively inhibiting human tumor cell lines overexpressing Pgp, or reducing nuclear Topo II catalytic activity with an IC50 of 9.8 to 18 nM. NPI-2358 concentration of 20 nM on human umbilical vein endothelial cells can rapidly induce tubulin depolymerization, and through the single cell layer. NPI-2358 acts on MM cells to stop the MM cells at the early stage of mitosis and induce cell death. NPI-2358 also inhibits microtubule formation, and migration of endothelial cells and MM cells, causing tumor vasculature to malfunction. NPI-2358 can induce cell death, does not affect the viability of other normal monocytes. NPI-2358 induces mitotic arrest or MM cell death, but blocking the JNK pathway can inactivate this induction. |
| In vivo study | On NPI-2358(7.5 mg/kg), the tumor growth was inhibited in mice bearing human plasma cell xenografts. NPI-2358 induced a decrease in tumor perfusion in a time and dose dependent manner. NPI-2358 acting on KHT sarcoma is more effective than acting on C3H tumor, and radiation treatment can enhance the anticancer activity of the two tumors. |
(3Z,6Z)-3-[(5-tert-Butyl-1H-imidazol-4-yl)methylene]-6-(phenylmethylene)-2,5-piperazinedione Plinabulin (NPI-2358) - Reference Information
| Application | (3Z,6Z)-3-[(5-tert-butyl-1h-imidazol-4-yl) methylene]-6-(benzylidene)-2, 5-piperazinedione, also known as Plinabulin(KPU-2,NPI-2358), was developed by Nereus pharmaceutical company, USA, it is a synthetic derivative of the low-molecular-ring dipeptide phenylahistin or halimide derived from marine Aspergillus, and is a tubulin-binding agent. |
| biological activity | plinablin (NPI-2358) is a vascular disrupting agent (VDA), it acts on tumor cells and affects tubulin depolymerization, with IC50 of 9.8-18 nM. Phase 1/2. |
| Target | TargetValue Tubulin 9.8 nM-18 nM |
| Target | Value |
| Tubulin | 9.8 nM-18 nM |
| in vitro study | NPI-2358 binds to the colchicine binding site of tubulin to effectively inhibit human tumor cell lines over-expressing Pgp, or reduce the catalytic activity of nuclear Topo II, IC50 9.8 to 18 nM. NPI-2358 concentration of 20 nM on human umbilical vein endothelial cells can rapidly induce tubulin depolymerization, and through the single cell layer. NPI-2358 acts on MM cells to stop the MM cells at the early stage of mitosis and induce cell death. NPI-2358 also inhibits microtubule formation, and migration of endothelial cells and MM cells, causing tumor vasculature to malfunction. NPI-2358 can induce cell death, does not affect the viability of other normal monocytes. NPI-2358 induces mitotic arrest or MM cell death, but blocking the JNK pathway can inactivate this induction. |
| in vivo study | NPI-2358(7.5 mg/kg) inhibited tumor growth in mice bearing human plasma cell xenografts. NPI-2358 induced a decrease in tumor perfusion in a time and dose dependent manner. NPI-2358 acting on KHT sarcoma is more effective than acting on C3H tumor, and radiation treatment can enhance the anticancer activity of the two tumors. |
Last Update：2024-04-09 20:02:46
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Product Name: Plinabulin (NPI-2358) Visit Supplier Webpage Request for quotationCAS: 714272-27-2
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Multiple Specifications
Product Name: Plinabulin (NPI-2358) Visit Supplier Webpage Request for quotationCAS: 714272-27-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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