Semaxinib | SU5416;NSC 696819;VEGFR 2 Kinase Inhibitor;Sugen 5416;Semaxanib | 塞马西尼 | Other Modeling Agents | VEGFR

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司马沙尼 /Semaxinib {[allProObj[0].p_purity_real_show]}

货号：A325242 同义名： 塞马西尼 / SU5416;NSC 696819

Semaxinib（SU5416）表现出对VEGFR（Flk-1/KDR）的强效和选择性抑制，IC50为1.23 μM。

Semaxinib 化学结构
CAS号：204005-46-9

Semaxinib 3D分子结构
CAS号：204005-46-9

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Semaxinib 纯度/质量文件产品仅供科研

货号：A325242 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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VEGFR 亚型比较

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	98%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	FGFR,PDGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	c-Kit,BTK	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		98%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			98%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	98+%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	98%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	98%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Semaxinib 生物活性

靶点	VEGFR2 VEGFR2/Flk1, IC50:1.23 μM
描述	Flk-1/KDR is one of the three vascular endothelial growth factor receptors (VEGFR) involved in angiogenesis. SU5416 is a potent, selective Flk-1/KDR inhibitor that inhibits the autophosphorylation and VEGF-dependent phosphorylation of Flk-1 receptor with IC50 values of 1.23 μM and 1.04 μM, respectively^[3]. SU5416 also potently inhibited Ret, Flk-3, ABL, ALKwith IC50 values of 0.17, 0.16, 11, and 1.2 μM, respectively. In the presence of 10μM SU5416, the residual activities of AMPK, CAMK-1, MKK1, and SKG are 43%, 67%, 23%, and 14%, respectively^[4]. In H526 cells cultured in serum-free medium for 24h in the presence of SCF or IGF-1, treatment with 10 μg/mL SU5416 largely decreased stem cell factor-stimulated VEGF mRNA expression and VEGF secretion^[5]. In subcutaneous tumor xenografts, SU5416 at the concentration of 1 - 25 mg/kg/day inhibited A375 tumor growth at a dose dependent manner. A >85% inhibitory effect on tumor growth was found after 38-day treatment of SU5416 at 25 mg/kg/day^[3].
作用机制	SU5416 is a 3-substituted indolin-2-one compound that blocks angiogenesis via inhibiting the catalysis of VEGFR^[3].

Semaxinib 动物研究

Dose	Rat: 5 mg/kg^[3] (i.v.); 20 mg/kg^[4] (s.c.) Mice: 100 mg/kg^[5] (s.c.); 25 mg/kg - 50 mg/kg^[6] (i.p.)
Administration	i.v., s.c., i.p.

Semaxinib 参考文献

[1]Happe CM, de Raaf MA, et al. Pneumonectomy combined with SU5416 induces severe pulmonary hypertension in rats. Am J Physiol Lung Cell Mol Physiol. 2016 Jun 1;310(11):L1088-97.

[2]Fong TA, Shawver LK, et al. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res. 1999 Jan 1;59(1):99-106.

[3]Fong TA, Shawver LK, Sun L, Tang C, App H, Powell TJ, Kim YH, Schreck R, Wang X, Risau W, Ullrich A, Hirth KP, McMahon G. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res. 1999 Jan 1;59(1):99-106.

[4]Mologni L, Sala E, Cazzaniga S, Rostagno R, Kuoni T, Puttini M, Bain J, Cleris L, Redaelli S, Riva B, Formelli F, Scapozza L, Gambacorti-Passerini C. Inhibition of RET tyrosine kinase by SU5416. J Mol Endocrinol. 2006 Oct;37(2):199-212.

[5]Litz J, Sakuntala Warshamana-Greene G, Sulanke G, Lipson KE, Krystal GW. The multi-targeted kinase inhibitor SU5416 inhibits small cell lung cancer growth and angiogenesis, in part by blocking Kit-mediated VEGF expression. Lung Cancer. 2004 Dec;46(3):283-91.

Semaxinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

4.20mL

0.84mL

0.42mL

20.98mL

4.20mL

2.10mL

41.97mL

8.39mL

4.20mL

Semaxinib 技术信息

CAS号	204005-46-9
分子式	C₁₅H₁₄N₂O
分子量	238.28

别名	塞马西尼 ;SU5416;NSC 696819;VEGFR 2 Kinase Inhibitor;Sugen 5416;Semaxanib
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 18 mg/mL(75.54 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 50 mg/mL(209.84 mM)，配合低频超声助溶

动物实验配方

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