KG5
作者：齐岳
发布时间：2023-08-22
09:22:17
点击数：
产品名称：KG5
产品描述：
| 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), 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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 95 mg/mL (206.77 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
