インジブリン
インジブリン 物理性質
- 比重(密度) :
- 1.31±0.1 g/cm3(Predicted)
- 貯蔵温度 :
- Sealed in dry,Store in freezer, under -20°C
- 溶解性:
- DMSO:33.25(Max Conc. mg/mL);85.29(Max Conc. mM)
- 外見 :
- A solid
- 酸解離定数(Pka):
- 9.38±0.70(Predicted)
- 色:
- Off-white to yellow
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01TOC3728 |
Indibulin |
204205-90-3 |
10mg |
￥62000 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01TOC3728 |
Indibulin |
204205-90-3 |
50mg |
￥258000 |
2024-03-01 |
購入 |
インジブリン 化学特性,用途語,生産方法
効能
抗悪性腫瘍薬, 微小管重合阻害薬
説明
Indibulin (D-24851; ZIO-301), a novel synthetic small molecule microtubule inhibitor, destabilizes microtubules and has antitumor activity but does not exhibit neurotoxicity in preclinical animal studies. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis. The drug can discriminate between highly posttranslationally modified tubulin present in mature neuronal microtubules, and less-modified tubulin present in immature neuronal or nonneuronal microtubules.
使用
Indibulin is a chemotherapeutic drug that destabilizes microtubules and is used to treat aggressive and heterogenous cancers, including breast cancer.
生物活性
Indibulin is a microtubule destabilizer that blocks tubulin polymerization (IC50 = 0.3 μM). Blocks cell cycle progression at metaphase and displays antitumor activity against a variety of malignancies in vitro (IC50 values ranging from 0.036 - 0.285 μM). Induces complete tumor remission in the Yoshida AH13 rat sarcoma model in vivo. Lacks neurotoxicity due to an ability to discriminate between posttranslationally modified tubulin in mature neuronal microtubules and less-modified tubulin present in immature neuronal or nonneuronal microtubules. Displays oral availability and efficacy towards MDR tumor cells.
Mode of action
Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines.
参考文献
Indibulin, a Novel Microtubule Inhibitor, Discriminates between Mature Neuronal and Nonneuronal Tubulinhttps://www.rndsystems.com/products/indibulin_3728https://pubchem.ncbi.nlm.nih.gov/compound/2929
インジブリン 上流と下流の製品情報
原材料
準備製品
インジブリン 生産企業
Global( 73)Suppliers
204205-90-3(インジブリン)キーワード:
- 204205-90-3
- Nascapine
- ZIO 301
- 2-(1-(4-Chlorophenylmethyl)-1H-indol-3-yl)-2-oxo-N-(pyridin-4-yl)acetamide
- Indibulin
- 2-[1-(4-Chlorobenzyl)-1H-indol-3-yl]-2-oxo-N-pyridin-4-ylacetamide
- lindiblin
- 2-[1-[(4-chlorophenyl)methyl]indol-3-yl]-2-oxo-N-pyridin-4-ylacetamide
- 1H-Indole-3-acetamide, 1-[(4-chlorophenyl)methyl]-α-oxo-N-4-pyridinyl-
- 2-(1-(4-Chlorophenylmethyl)-1H-indol-3-yl)-2-oxo-N-(pyridin-4-yl)acetamide ISO 9001：2015 REACH
- Indibulin,Apoptosis,ZIO301,D24851,Inhibitor,inhibit,ZIO-301,D-24851,Microtubule/Tubulin
- インジブリン