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KRN-633
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KRN-633图片
CAS NO:286370-15-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
N-[2-氯-4-[(6,7-二甲氧基-4-喹唑啉基)氧基]苯基]-N'-丙基脲
KRN633
产品介绍
KRN633 是一种 VEGFR 抑制剂,能够一种 VEGFR1 (IC50:170 nM)、VEGFR2 (IC50:160 nM)、VEGFR3 (IC50:125 nM)。

产品描述

KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633 for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively.

体外活性

In human umbilical vein endothelial cells, KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β with IC50 of 11.7, 1.16, 8.01, 130 nM, respectively. In endothelial cells, KRN-633 inhibits the formation of the capillary tube. KRN-633 suppress the VEGF-driven proliferation of HUVECs (IC50=14.9 nM).

体内活性

In athymic mouse and rat xenograft models, KRN-633 was able to inhibit tumor growth in various tissue sources such as lungs, colon, and prostate. It was also observed that in the non-necrosis region of tumor grafts, the number of endothelial cells was reduced and vascular permeability decreased. In the regenerated tumors, KRN-633 can also ablate tumor growth.

激酶实验

In cell-free kinase assays,with1 μM ATP the IC50 of KRN-633 is from 0.3 nM to 10 μM.

细胞实验

Cancer cells, such as A549, Ls174T, HT29, DU145, LNCap, and PC-3 cells, are cultured for 24 hours, then add KRN-633 (0.01 to 10 μM)that is prepared in 0.1% DMSO in the medium growing for 96 hours.

动物实验

In tumor xenografts mice model, are treated with KRN-633(10-100 mg/kg) once or twice per day. In human tumor xenografts athymic rats (BALB/cA, Jcl-nu), when the tumors reach the average size indicated (162 to 657 mm3), and are treated with KRN-633 either once or twice per day. After 14days treatment, Calculate the tumor growth inhibition.

Cas No.

286370-15-8

分子式

C20H21ClN4O4

分子量

416.86

别名

N-[2-氯-4-[(6,7-二甲氧基-4-喹唑啉基)氧基]苯基]-N'-丙基脲;KRN633

储存和溶解度

DMSO:8 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years