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。
| 生物活性 | KG5 is an orally active dualPDGFRβandB-Rafallosteric inhibitor. KG5 also inhibitsFlt3,KITandc-Raf. KG5 has anticancer, antiangiogenic activities[1]. |
| IC50& Target[1] | PDGFRβ 520 nM (Kd) | PDGFRα 300 nM (Kd) | B-Raf | c-Raf | FLT3 52 nM (Kd) | KIT 170 nM (Kd) |
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体外研究
(In Vitro) | KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) and endothelial cells viability with EC50values of 0.59 μM and 0.54 μM, respectively[1].
Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259[1].
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[1].
KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK and ERK in endothelial cells stimulated with bFGF or VEGF[1].
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体内研究
(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[1].
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 Cmaxof 3.6 μg/mL, T1/2of 11.5 h, and an area under the concentration time curve (AUC0-12h) of 14.7 μgoh/mL[1].
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis[1].
| Animal Model: | Male Nu/Nu mice injected with SN12C-RFP cells[1] | | Dosage: | 100 mg/kg | | Administration: | Oral administration; daily; for 26 days | | Result: | Prevented tumor growth in an orthotopic renal cell carcinoma model. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(217.65 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1765 mL | 10.8826 mL | 21.7652 mL | | 5 mM | 0.4353 mL | 2.1765 mL | 4.3530 mL | | 10 mM | 0.2177 mL | 1.0883 mL | 2.1765 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.44 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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