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CAS No.: 874819-74-6

Toceranib phosphate/托西尼布磷酸盐 Catalog No. CSN17231

Synonyms: SU11654 phosphate;PHA 291639E phosphate;PHA-291639 Phosphate

Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PDGFRβ

Ki:5nM VEGFR2

Ki:6nM
描述Many of the processes involved in tumor growth, progression, and metastasis are mediated by ligand-receptor interactions involving RTKs (receptor tyrosine kinases) and downstream signaling molecules. Because of the demonstrated importance of RTKs in the control of many cellular processes (particularly proliferation) and the role of aberrant RTK signaling in cancer, RTKs have emerged as important targets for the development of anticancer therapies. Toceranib Phosphate is the phosphate form of Toceranib. Toceranib, a small molecule with an indolinone chemical structure, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit. In vitro, toceranib exerted a potent antiproliferative effect on endothelial cells. Additionally, toceranib treatment could induce cell cycle arrest and subsequent apoptosis in tumor cell lines expressing activating mutations in split kinase RTKs. In mouse xenograft models, oral administration of toceranib affected the growth of multiple tumor cell lines originating from a variety of tissues, leading to either tumor regression or tumor growth inhibition. On the basis of preclinical work in rodent models, the therapeutic range of toceranib for target inhibition was considered to be 50–100 ng/ml for 12 h of a 24-h dosing period^[3].
参考文献

[1] London C, Mathie T, et al. Preliminary evidence for biologic activity of toceranib phosphate) in solid tumours. Vet Comp Oncol. 2012 Sep;10(3):194-205.
[2] Yancey MF, Merritt DA, et al. Pharmacokinetic properties of toceranib phosphate (Palladia, SU11654), a novel tyrosine kinase inhibitor, in laboratory dogs and dogs with mast cell tumors. J Vet Pharmacol Ther. 2010 Apr;33(2):162-71.
[3] Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies

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
- 2.0224 mL
- 10.1122 mL
- 20.2244 mL
- 5 mM
- 0.4045 mL
- 2.0224 mL
- 4.0449 mL
- 10 mM
- 0.2022 mL
- 1.0112 mL
- 2.0224 mL

技术信息

CAS号

874819-74-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H28FN4O6P

运输

蓝冰

分子量

494.45

别名

SU11654 phosphate;PHA 291639E phosphate;PHA-291639 Phosphate;托西尼布磷酸盐

溶解度

DMSO	2.0 mg/mL (4.0 mM)
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
PDGFRβ		Ki:5nM
VEGFR2		Ki:6nM

Toceranib phosphate/托西尼布磷酸盐 Catalog No. CSN17231

靶点选择性

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