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CAS No.: 356068-94-5

Toceranib/托西尼布 Catalog No. CSN15964

Synonyms: SU11654;PHA 291639E;PHA-291639

Toceranib 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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技术信息

生物活性

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, 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].
作用机制Toceranib competes directly with ATP at the intracellular kinase domain of the RTK, thus preventing tyrosine phosphorylation and subsequent signal transduction^[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
- 2.5223 mL
- 12.6117 mL
- 25.2234 mL
- 5 mM
- 0.5045 mL
- 2.5223 mL
- 5.0447 mL
- 10 mM
- 0.2522 mL
- 1.2612 mL
- 2.5223 mL

技术信息

CAS号

356068-94-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H25FN4O2

运输

蓝冰

分子量

396.46

别名

SU11654;PHA 291639E;PHA-291639;托西尼布

溶解度

DMSO	2.0 mg/mL (5.0 mM) warming
Water	Insoluble

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