Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KG5 是 PDGFRβ 和 B-Raf 的双重变构抑制剂,对 PDGFRβ 和 PDGFRα 的 Kd 分别为 520 nM 和 300 nM。 KG5 抑制 FLT3、KIT 和 c-Raf,具有抗癌和抗血管生成活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 478 | 现货 | ||
5 mg | ¥ 1,130 | 现货 | ||
10 mg | ¥ 1,800 | 现货 | ||
25 mg | ¥ 3,680 | 现货 | ||
50 mg | ¥ 5,330 | 现货 | ||
100 mg | ¥ 7,530 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,330 | 现货 |
产品描述 | KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities. |
靶点活性 | FLT3:52 nM (Kd), PDGFRβ:520 nM (Kd), PDGFRα:300 nM (Kd), c-Kit:170 nM (Kd) |
体外活性 | KG5 inhibits FLT3 and KIT at 52 and 170 nM, respectively. In endothelial cells stimulated with bFGF or VEGF, KG5 (5 μM) inhibits phosphorylation of MEK and ERK. KG5 inhibits vascular smooth muscle cells (VSMCs) and endothelial cell viability with EC50 values of 0.59 μM and 0.54 μM, respectively. KG5 selectively blocks S338 phosphorylation, yet does not influence S259[1]. |
体内活性 | KG5 (1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis. In male Nu/Nu mice injected with SN12C-RFP cells, KG5 (100 mg/kg; oral) prevents tumor growth. KG5 (50 mg/kg; i.p.) completely blocks angiogenesis in mice injected with Matrigel containing bFGF with a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an AUC0-12h of 14.7 μg•h/mL[1]. |
分子量 | 459.45 |
分子式 | C20H16F3N7OS |
CAS No. | 877874-85-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (206.77 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1765 mL | 10.8826 mL | 21.7652 mL | 54.4129 mL |
5 mM | 0.4353 mL | 2.1765 mL | 4.353 mL | 10.8826 mL | |
10 mM | 0.2177 mL | 1.0883 mL | 2.1765 mL | 5.4413 mL | |
20 mM | 0.1088 mL | 0.5441 mL | 1.0883 mL | 2.7206 mL | |
50 mM | 0.0435 mL | 0.2177 mL | 0.4353 mL | 1.0883 mL | |
100 mM | 0.0218 mL | 0.1088 mL | 0.2177 mL | 0.5441 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
KG5 877874-85-6 Angiogenesis MAPK Tyrosine Kinase/Adaptors Raf FLT PDGFR c-Kit B-Raf antiangiogenic KIT CD135 Raf kinases Cluster of differentiation antigen 135 Platelet-derived growth factor receptor Fms like tyrosine kinase 3 metastasis c-Raf FLT3 PDGFRβ inhibit anticancer phosphorylation SCFR Inhibitor KG 5 KG-5 CD117 inhibitor