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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
BAY 73-4506 monohydrate
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- 规格:
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg/200 mg/500 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥261.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥237.0 |
| 规格: | 10 mg | 产品价格: | ¥380.0 |
| 规格: | 25 mg | 产品价格: | ¥644.0 |
| 规格: | 50 mg | 产品价格: | ¥950.0 |
| 规格: | 100 mg | 产品价格: | ¥1500.0 |
| 规格: | 200 mg | 产品价格: | ¥2238.0 |
| 规格: | 500 mg | 产品价格: | ¥3700.0 |
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Regorafenib monohydrate
CAS No. : 1019206-88-2
MCE 国际站:Regorafenib monohydrate
产品活性:Regorafenib (BAY 73-4506) monohydrate 是一种口服有效的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂,抑制 VEGFR1/2/3,PDGFRβ,Kit,RET 和 Raf-1 的 IC50 分别为 13/4.2/46,22,7,1.5 和 2.5 nM。Regorafenib monohydrate 显示出非常强的抗肿瘤和抗血管生成活性。
研究领域:Protein Tyrosine Kinase/RTK | Autophagy | MAPK/ERK Pathway
作用靶点:VEGFR | Autophagy | PDGFR | Raf | RET | FGFR | c-Kit | Tie
In Vitro: Regorafenib monohydrate (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells.
Regorafenib monohydrate (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2.
Regorafenib monohydrate causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.
In Vivo: Regorafenib monohydrate (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model.
Regorafenib monohydrate (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model.
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