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CAS No.: 1433953-83-3

SAR131675 Catalog No. CSN17854

SAR131675 is selective inhibitor of VEGFR3 with IC50 and Ki of 23 nM, 12 nM, respectively.

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400-920-2911

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实验方案

技术信息

生物活性

描述One key molecule mediating tumor lymphangiogenesis is the VEGF receptor-3 (VEGFR-3), a tyrosine kinase receptor recognized and activated by VEGFC and VEGFD, commonly expressed in malignant and tumor-infiltrating stromal cells^[3]. SAR131675 is a potent and selective VEGFR-3 inhibitor which inhibits VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC₅₀ values of 20 and 45 nmol/L, respectively. SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC₅₀ of about 20 nmol/L^[3]. SAR131675 is well tolerated in mice and shows a potent antitumoral effect in several orthotopic and syngenic models, including mammary 4T1 carcinoma and RIP1.Tag2 tumors. Interestingly, it significantly reduces lymph node invasion and lung metastasis, showing its antilymphangiogenic activity in vivo. Moreover, SAR131675 significantly reduces TAM (tumor-associated macrophages) infiltration and aggregation in 4T1 tumors^[3].
参考文献

[1] Nicolas E, Pauline B, et al. Specific Inhibition of the VEGFR-3 Tyrosine Kinase by SAR131675 Reduces Peripheral and Tumor Associated Immunosuppressive Myeloid Cells. Cancers (Basel). 2014 Mar; 6(1): 472–490.
[2] Alam A, Blanc I, et al. SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. Mol Cancer Ther. 2012 Aug;11(8):1637-49.
[3] Alam A, Blanc I, Gueguen-Dorbes G, Duclos O, Bonnin J, Barron P, Laplace MC, Morin G, Gaujarengues F, Dol F, Hérault JP, Schaeffer P, Savi P, Bono F. SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. Mol Cancer Ther. 2012 Aug;11(8):1637-49. doi: 10.1158/1535-7163.MCT-11-0866-T. Epub 2012 May 14. PMID: 22584122.

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
- 2.7902 mL
- 13.9512 mL
- 27.9024 mL
- 5 mM
- 0.5580 mL
- 2.7902 mL
- 5.5805 mL
- 10 mM
- 0.2790 mL
- 1.3951 mL
- 2.7902 mL

技术信息

CAS号

1433953-83-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H22N4O4

运输

蓝冰

分子量

358.39

别名

溶解度

DMSO	72.0 mg/mL (200.9 mM)
Water	insoluble

动物实验配方

5% DMSO+30% PEG 300+5% Tween 80+water

3 mg/mL

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