|N-[2-氯-4-[(6,7-二甲氧基-4-喹唑啉基)氧基]苯基]-N'-丙基脲|CsnPharm

CAS No.: 286370-15-8

KRN-633 Catalog No. CSN15848

Synonyms: KRN-633

KRN-633 can inhibit VEGFR1, VEGFR2 and VEGFR3 with IC50 of 170 nM, 160 nM, and 125 nM, respectively.

规格	价格	促销价格	库存	数量

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 VEGFR3

IC50:125nM VEGFR2

IC50:160nM VEGFR1

IC50:170nM
描述The vascular endothelial growth factor (VEGF)-VEGF receptor (R) system is deeply involved in angiogenesis and lymphangiogenesis^[3]. KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β (IC50=11.7, 1.16, 8.01, 130 nM) in human umbilical vein endothelial cells. KRN-633 also inhibits the VEGF-driven proliferation of HUVECs (IC50=14.9 nM). KRN-633 suppresses capillary tube formation of endothelial cells. KRN-633 inhibits tumor growth in several tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN-633 also causes the regression of some well-established tumors and those that have regrown after the cessation of treatment. KRN-633 is well tolerated and has no significant effects on body weight or the general health of the animals. Histologic analysis of tumor xenografts treated with KRN-633 reveals a reduction in the number of endothelial cells in non-necrotic areas and a decrease in vascular permeability^[4]. Reduction in the expression levels of VEGF and VEGF receptor-2 in the CL precedes the impairment of luteal circulation and a series of events leading to parturition (i.e., reduction of plasma progesterone, enhancement of myometrium contractility, and onset of parturition). Blocking of VEGF signaling by using the inhibitor of VEGFR tyrosine kinase KRN633 at mid-pregnancy caused a similar sequence of events and induced preterm birth^[5]. In retinas of rats injected subcutaneously with KRN633 (10 mg/kg), simplified vasculature attributable to capillary regression and prevention of endothelial cell growth were seen, whereas no visible changes in the morphology of the retinal layers were observed^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3989 mL
- 11.9944 mL
- 23.9889 mL
- 5 mM
- 0.4798 mL
- 2.3989 mL
- 4.7978 mL
- 10 mM
- 0.2399 mL
- 1.1994 mL
- 2.3989 mL

技术信息

CAS号

286370-15-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H21ClN4O4

运输

蓝冰

分子量

416.86

别名

KRN-633

溶解度

DMSO	9.0 mg/mL (21.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

0.5% methylcellulose+0.2% Tween 80+water

10 mg/mL

suspension

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靶点	Description	IC50
VEGFR3		IC50:125nM
VEGFR2		IC50:160nM
VEGFR1		IC50:170nM

KRN-633 Catalog No. CSN15848

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