|(Z)-3-((3,5-二甲基-1H-吡咯-2-基)亚甲基)二氢吲哚-2-酮|CsnPharm

CAS No.: 194413-58-6

(Z)-司马沙尼 Catalog No. CSN15794

Synonyms: (Z)-SU5416;Z-SU-5416;SU-5416

Semaxanib is an inhibitor of VEGFR2 (namely Flk-1 or KDR) with IC50 of 1.23 μM.

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技术信息

生物活性

描述Vascular endothelial growth factor (VEGF) plays a prosurvival and antiapoptotic role in endothelial cells. Z-Semaxanib (SU5416) is the first VEGF receptor 2 inhibitor to enter clinical development for cancer therapy^[3]. SU5416 directly inhibited VEGF-mediated ERK phosphorylation, cell proliferation, and Kdr transcription, but not Matrigel tube formation in primary murine cardiac endothelial cells in vitro. SU5416 did not inhibit chronic hypoxia (CH-PH) induced Right ventricular(RV) angiogenesis, endothelial cell proliferation, or RV hypertrophy in vivo, despite significantly altering the expression profile of genes involved in angiogenesis^[4]. The combination of radiation and SU5416 significantly inhibited cell survival, the repair of radiation-induced DNA damage, and induced apoptosis. It also caused cell cycle arrest, inhibited cell migration and invasion, and suppressed angiogenesis^[5]. SU5416 inhibited VEGF expression at the transcriptional level through the HIF-1 DNA binding site. HIF-1 is composed of HIF-1alpha and HIF-1beta subunits. SU5416 specifically decreased HIF-1alpha, but not HIF-1beta protein levels, it inhibited VEGF and HIF-1alpha expression through the inhibition of PI3K/AKT/p70S6K1 pathway in ovarian cancer cells^[6]. SU5416 potently activated AhR-dependent reporter genes, induced AhR nuclear localization, facilitated AhR-DNA binding, and increased, expression of its endogenous target genes. SU5416 significantly inhibited proliferation of Hepa1 hepatoma cells in an AhR-dependent manner, but did not induce apoptosis. SU5416 also inhibited the growth of human HepG2 liver cancer cells^[7].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A431 cells	-	Function assay	-	Inhibition of VEGFR2 expressed in human A431 cells, IC50=12.9 μM	20558072
CHO cells	-	Function assay	-	Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells, IC50=0.884 μM	12477352
human A431 cells	-	Function assay	-	Antiangiogenic activity against human A431 cells, IC50=0.085 μM	20403693

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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
- 4.1967 mL
- 20.9833 mL
- 41.9666 mL
- 5 mM
- 0.8393 mL
- 4.1967 mL
- 8.3933 mL
- 10 mM
- 0.4197 mL
- 2.0983 mL
- 4.1967 mL

技术信息

CAS号

194413-58-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H14N2O

运输

蓝冰

分子量

238.28

别名

(Z)-SU5416;Z-SU-5416;SU-5416

溶解度

DMSO	45.0 mg/mL (188.8 mM) warming
Water	insoluble

动物实验配方

5% DMSO+40%PEG 300+ 5% Tween80 + water

0.5 mg/mL

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A431 cells	-	Function assay	-	Inhibition of VEGFR2 expressed in human A431 cells, IC50=12.9 μM	20558072
CHO cells	-	Function assay	-	Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells, IC50=0.884 μM	12477352
human A431 cells	-	Function assay	-	Antiangiogenic activity against human A431 cells, IC50=0.085 μM	20403693
human HeLa cells	-	Proliferation assay	4 days	Antiproliferative activity against human HeLa cells after 4 days by coulter counter method, IC50=20 μM	23124213
human HMEC1 cells	-	Proliferation assay	7 days	Antiproliferative activity against human HMEC1 cells after 7 days by coulter counter method, IC50=15 μM	23124213
human MCF7 cells	-	Proliferation assay	4 days	Antiproliferative activity against human MCF7 cells after 4 days by coulter counter method, IC50=1.9 μM	23124213
human SF539 cells	-	Function assay	-	Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine ELISA, IC50=2.4 μM	19748785
human U251 cells	-	Function assay	-	Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50=12.9 nM	24900865
HUVEC cells	-	Proliferation assay	72 h	Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by trypan blue assay, GI50=13.6 μM	26318056
MCF7 cells	-	Cytotoxicity assay	48 h	Cytotoxicity against human MCF7 cells after 48 hrs by CCK8 assay, IC50=3.1 nM	23777898
mouse B16F10 cells	-	Cytotoxicity assay	48 h	Cytotoxicity against mouse B16F10 cells after 48 hrs by CCK8 assay, IC50=3.6 nM	23777898

(Z)-司马沙尼 Catalog No. CSN15794

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