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。

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.

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PDGFRβ 520 nM (Kd) PDGFRα 300 nM (Kd)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Eric A Murphy, et al. Disruption of angiogenesis and tumor growth with an orally active drug that stabilizes the inactive state of PDGFRbeta/B-RAF. Proc Natl Acad Sci U S A. 2010 Mar 2;107(9):4299-304.

In Vitro: DMSO : 100 mg/mL (217.65 mM; Need ultrasonic)配制储备液