SKLB1002

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Chemical Structure| 1225451-84-2 同义名 : -
CAS号 : 1225451-84-2
货号 : A300860
分子式 : C13H12N4O2S2
纯度 : 99%
分子量 : 320.39
MDL号 : MFCD27938707
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • VEGFR2

    VEGFR2, IC50:32 nM
描述 SKLB1002 is a potent inhibitor of VEGF receptor 2 signaling. SKLB1002 administration significantly reduced endothelial cell proliferation, migration and tube formation in vitro. Mechanistically, SKLB1002 inhibited endothelial angiogenic functions by blocking the phosphorylation of ERK1/2, JNK and p38[3]. Compared with the solvent control, administration of 100 mg/kg/d SKLB1002 reached more than 60% inhibition against human tumor xenografts in athymic mice[4]. Inhibition of VEGF signalling using SKLB1002 increased ROBO4 (Roundabout-4) expression and reduced neovascularisation indices. Furthermore, SKLB1002 significantly decreased ROBO4-β3 integrin interaction in diabetes[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.21mL

6.24mL

3.12mL
参考文献

[1]Nie W, Ma XL, et al. Synergic antitumor effect of SKLB1002 and local hyperthermia in 4T1 and CT26. Clin Exp Med. 2014 May;14(2):203-13.

[2]Zhang S, Cao Z, et al. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res. 2011 Jul 1;17(13):4439-50.

[3]Zhang QY, Tao SY, Lu C, Li JJ, Li XM, Yao J, Jiang Q, Yan B. SKLB1002, a potent inhibitor of VEGF receptor 2 signaling, inhibits endothelial angiogenic function in vitro and ocular angiogenesis in vivo. Mol Med Rep. 2020 Jun;21(6):2571-2579

[4]Zhang S, Cao Z, Tian H, Shen G, Ma Y, Xie H, Liu Y, Zhao C, Deng S, Yang Y, Zheng R, Li W, Zhang N, Liu S, Wang W, Dai L, Shi S, Cheng L, Pan Y, Feng S, Zhao X, Deng H, Yang S, Wei Y. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res. 2011 Jul 1;17(13):4439-50

[5]Abdelsaid M, Coucha M, Hafez S, Yasir A, Johnson MH, Ergul A. Enhanced VEGF signalling mediates cerebral neovascularisation via downregulation of guidance protein ROBO4 in a rat model of diabetes. Diabetologia. 2017 Apr;60(4):740-750