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- 文献和实验
- 技术资料
- CAS号：
714272-27-2
- 规格：
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥308.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥888.0 |
| 规格： | 2mg | 产品价格： | ￥418.0 |
| 规格： | 5mg | 产品价格： | ￥789.0 |
| 规格： | 10mg | 产品价格： | ￥1560.0 |
| 规格： | 25mg | 产品价格： | ￥2632.0 |
| 规格： | 50mg | 产品价格： | ￥3776.0 |
| 规格： | 100mg | 产品价格： | ￥5272.0 |
| 规格： | 200mg | 产品价格： | ￥7104.0 |
Product Introduction
Bioactivity
| 名称 | Plinabulin |
| 描述 | Plinabulin (NPI-2358) (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing tumor cells ( IC50: 9.8-18 nM). Plinabulin selectively targets and binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics. This disrupts mitotic spindle assembly leading to cell cycle arrest at M phase and blockage of cell division. |
| 细胞实验 | The adherent cells are plated in 96-well flat-bottomed plates and allowed to attach for 24 hours at 37 °C. HL-60 and HL-60/MX2 cells are plated in 96-well plates on the day of NPI-2358 addition. Serially diluted NPI-2358 is added to cells at concentrations ranging from 2 pM to 20 μM. Cells treated with a final concentration of 0.25% (v/v) DMSO serves as the vehicle control. Cell viability is assessed 48 hours later by measuring the reduction of resazurin with a fluorimeter. The IC50 value is calculated.(Only for Reference) |
| 体外活性 | NPI-2358时间和剂量依赖性地诱导肿瘤灌注降低.在携带人浆细胞移植瘤的鼠中,NPI-2358（7.5 mg/kg）可抑制肿瘤生长.与对C3H肿瘤的效果相比,NPI-2358对KHT肉瘤的作用更好,辐射处理可以增强对两种肿瘤的抗癌活性. |
| 体内活性 | 在人脐静脉内皮细胞中,NPI-2358（20 nM）可快速诱导微管蛋白解聚,并透过单细胞层。NPI-2358可使MM细胞停在有丝分裂早期,并诱导细胞死亡。NPI-2358与微管蛋白的秋水仙素结合位点结合,可有效抑制过量表达Pgp的人肿瘤细胞系,或使核Topo II催化活性降低（IC50：9.8-18 nM）。NPI-2358也还抑制微管形成及内皮细胞和MM细胞的迁移,造成肿瘤脉管系统功能失常。NPI-2358对有丝分裂停滞或MM细胞死亡具有诱导作用,但通过阻断JNK通路可使该作用失活。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.95 mM), Sonication is recommended. DMSO : 50 mg/mL (148.64 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | Tubulin | Plinabulin | NPI2358 | NPI 2358 | MicrotubuleAssociated | Microtubule/Tubulin | Microtubule Associated | Inhibitor | inhibit |
| 相关产品 | 4-Isopropoxybenzoic acid | α-Cyclodextrin | Mebendazole | Flubendazole | Oxfendazole | Methylene Blue trihydrate | N-Phenylbenzylamine | Colchicine | Pregnenolone acetate | Paclitaxel | 4'-Demethylepipodophyllotoxin | Albendazole |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Failed Clinical Trials Compound Library | Anti-Lung Cancer Compound Library | Microtubule-Targeted Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Target-Focused Phenotypic Screening Library | Anti-Cancer Drug Library |
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普那布林【714272-27-2】
￥308 - 7104
