产品
编 号：F493764
分子式：C20H16F3N7OS
分子量：459.45
分子式：C20H16F3N7OS
分子量：459.45
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 877874-85-6
产品详情
生物活性：
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
体内研究：
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.Animal Model:Male Nu/Nu mice injected with SN12C-RFP cells
Dosage:100 mg/kg
Administration:Oral administration; daily; for 26 days
Result:Prevented tumor growth in an orthotopic renal cell carcinoma model.
体外研究：
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.
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
体内研究：
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.Animal Model:Male Nu/Nu mice injected with SN12C-RFP cells
Dosage:100 mg/kg
Administration:Oral administration; daily; for 26 days
Result:Prevented tumor growth in an orthotopic renal cell carcinoma model.
体外研究：
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.
产品资料
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