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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 K_ds 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 C_max of 3.6 μg/mL, T_1/2 of 11.5 h, and an area under the concentration time curve (AUC_0-12h) of 14.7 μg•h/mL.
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis.

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