产品说明书

SAR131675

Print
Chemical Structure| 1433953-83-3 同义名 : -
CAS号 : 1433953-83-3
货号 : A342706
分子式 : C18H22N4O4
纯度 : 99%+
分子量 : 358.392
MDL号 : MFCD23098773
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(292.98 mM)，配合低频超声，并水浴加热至45℃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
动物实验配方：

5% DMSO+30% PEG 300+5% Tween 80+water 3 mg/mL

生物活性
靶点

  • VEGFR3

    VEGFR3, IC50:23 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.95mL

2.79mL

1.40mL

27.90mL

5.58mL

2.79mL
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.