KG5
作者：齊岳
發布時間：2023-08-22
09:22:17
點擊數：
產品名稱：KG5
產品描述：
| 產品描述 | 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. |
| 靶點活性 | FLT3:52 nM (Kd), PDGFRβ:520 nM (Kd), PDGFRα:300 nM (Kd), Kit:170 nM (Kd) |
| 體外活性 | 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]. |
| 體內活性 | 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 |
存儲
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 )
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公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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