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- MedChemExpress(MCE)
- 美国
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- 2025年12月05日
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- 文献和实验
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4°C, protect from light
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
877874-85-6
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥857.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥359.0 |
| 规格： | 5 mg | 产品价格： | ￥848.0 |
| 规格： | 10 mg | 产品价格： | ￥1350.0 |
| 规格： | 25 mg | 产品价格： | ￥2750.0 |
| 规格： | 50 mg | 产品价格： | ￥3988.0 |
| 规格： | 100 mg | 产品价格： | ￥5638.0 |
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KG5
CAS No. : 877874-85-6
MCE 国际站：KG5
产品活性：KG5 是一种具有口服活性的双重 PDGFRβ 和 B-Raf 变构抑制剂。KG5 还抑制 Flt3，KIT 和 c-Raf，并具有抗癌，抗血管生成活性。
研究领域：MAPK/ERK Pathway | Protein Tyrosine Kinase/RTK
作用靶点：Raf | PDGFR | FLT3 | c-Kit
In Vitro: KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) and endothelial cells viability with EC50 values of 0.59 μM and 0.54 μM, respectively.
Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259.
KG5 (Compound 6) inhibits only PDGFRα and β with Kds of 300 and 520 nM, respectively, and Flt3 and KIT at 52 and 170 nM, respectively.
KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK and ERK in endothelial cells stimulated with bFGF or VEGF.
In Vivo: KG5 (Compound 6; 100 mg/kg; oral administration; daily; for 26 days) treatment prevents tumor growth in an orthotopic renal cell carcinoma model.
KG5 (Compound 6; 50 mg/kg; i.p.; twice daily) treatment completely blocks angiogenesis relative to vehicle control in mice (injected with Matrigel containing bFGF). Pharmacokinetic analysis of the dose and formulation of KG5 used indicated a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an area under the concentration time curve (AUC0-12h) of 14.7 μg•h/mL.
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis.
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文献和实验-150(145) 21.81 兔1.36-2.26kg 28.4-85.1/kg(150) 60-140/kg(300) 132.609.75 金黄地鼠(成
) 7.1-14.2 10-15 黑猩猩(成) 140-410/kg 0.5-11 豚鼠(成) 21.2-85.0 15-75 猕猴(成) 110-300/kg
0.54 0.30 0.85 0.94 0.59 0.02 0.01 0.00070.0008 0.10 0.2 0.2 猫 3.3kg
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