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Semaxinib

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Chemical Structure| 204005-46-9 同义名 : 塞马西尼 ;SU5416;NSC 696819;VEGFR 2 Kinase Inhibitor;Sugen 5416;Semaxanib
CAS号 : 204005-46-9
货号 : A325242
分子式 : C15H14N2O
纯度 : 98%
分子量 : 238.28
MDL号 : MFCD09763655
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.