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Vatalanib 2HCl

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Chemical Structure| 212141-51-0 同义名 : CGP-797870 dihydrochloride;ZK-222584 dihydrochloride;CGP-7978.;PTK787/ZK 222584;CGP79787D;ZK-232934;CGP-797870;ZK 222584;PTK/ZK;PTK787;CGP 79787;Vatalanib (hydrochloride);ZK 222584 2HCl;PTK787 dihydrochloride;Vatalanib dihydrochloride
CAS号 : 212141-51-0
货号 : A392716
分子式 : C20H17Cl3N4
纯度 : 99%+
分子量 : 419.735
MDL号 : MFCD08458964
存储条件：

粉末 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: 50 mg/mL(119.12 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

H2O: 50 mg/mL(119.12 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 70 mg/mL suspension

生物活性
靶点

  • VEGFR1

    VEGFR1/FLT1, IC50:77 nM

  • VEGFR3

    VEGFR3/FLT4, IC50:660 nM

  • VEGFR2

    VEGFR2/KDR, IC50:37 nM

    VEGFR2/Flk1, IC50:270 nM
描述 Vatalanib dihydrochloride is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.91mL

2.38mL

1.19mL

23.82mL

4.76mL

2.38mL
参考文献

[1]Murakami M, Kobayashi S, et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011 Feb;18(2):589-96.

[2]Wood JM, Bold G, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000 Apr 15;60(8):2178-89.