Semaxanib (SU5416)

Dangerous Goods

CAS number：194413-58-6 molecular formula：C15H14N2O

overview

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physicochemical properties

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MSDS

overview

compound introduction

Information Semaxanib (SU5416) is a potent and selectiveVEGFR(Flk-1/KDR) inhibitor withIC50of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3. Targets VEGFR2/Flk1 (Cell-free assay) 1.23 μM In vitro Semaxanib inhibits VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with IC50 of 1.04 μM. Semaxanib inhibits PDGF-dependent autophosphorylation in NIH 3T3 cells with IC50 of 20.3 μM. Semaxanib inhibits VEGF- and FGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 and 50 μM, respectively. Semaxanib treatment has no effect on the in vitro growth of C6 glioma, Calu 6 lung carcinoma, A375 melanoma, A431 epidermoid carcinoma, and SF767T glioma cells (all IC50s > 20 μM). In vivo Semaxanib dose-related inhibits growth of A375 tumor in vivo. A >85% inhibition of subcutaneous tumor growth is observed with daily i.p. administration of SU5416 in DMSO at Semaxanib, without measurable toxicity. Semaxanib shows broad spectrum antitumor activity. SU5416 significantly inhibits the subcutaneous growth of 8 of 10 tumor lines tested (A431, Calu-6, C6, LNCAP, EPH4-VEGF, 3T3HER2, 488G2M2 and SF763T cells) with an average mortality rate of 2.5%. Semaxanib (25 mg/kg/day) displays potent antiangiogenic activity, resulting in a significant reduction of both the total and functional vascular density of the tumor microvasculature. Cell Research(from reference) Cell lines：HUVECs Concentrations：~100 μM Incubation Time：2 days

Specs

Chinese alias	司马沙尼 (SU5416)
English alias	(Z)-Semaxinib \| BRN 0844684 \| CAS-204005-46-9 \| NCGC00094381-01 \| SCHEMBL194769 \| SCHEMBL19571 \| SU005416 \| Lopac0_001110 \| (Z)-SU 5416 \| NCGC00094381-19 \| Sugen 5416 \| HMS3648O12 \| HY-10374 \| MLS001304019 \| TSU 16 \| WUWDLXZGHZSWQZ-WQLSENKSSA-N \| ES-0010
CAS number	194413-58-6	molecular formula	C15H14N2O
molecular weight	238.28 g/mol	Exact mass	-
PSA	44.900 Å²	logp	2.5

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Safety information

pictogram：

GHS07

Signal word：

Warning

Hazard Statement：

H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激

Statement of Preventive Measures：

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P304+P340: 如误吸入：将人转移