|1,2,4,5-苯四胺四盐酸盐|CsnPharm

CAS No.: 4506-66-5

Benzene-1,2,4,5-tetraamine tetrahydrochloride Catalog No. CSN17077

Synonyms: FAK Inhibitor 14;FAK Inhibitor Y15;Focal Adhesion Kinase Inhibitor 14

Y15 is a small molecule FAK phosphorylation inhibitor which specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.

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实验方案

技术信息

生物活性

描述FAK (Focal adhesion kinase), a non-receptor tyrosine kinase, can regulate the cytoskeleton and act as a scaffolding and signaling protein for other adhesion molecules. The expression of FAK and its phosphorylation status show a strong correlation with the invasive phenotype of aggressive human tumors. Y15 is a selective FAK inhibitor^[1]. Treatment with Y15 caused decrease of p-FAK-Y397 in TT thyroid cancer cells at concentration of 1μM and 3μM, as well as decrease of both p-FAK-Y397 and FAK expression in TPC1, K1 and BCPAP thyroid cancer cells dose-dependently at concentration ranging 5-50μM. The cell viability showed that Y15 was much potent than Defactinib on growth inhibition of the four thyroid cancer cell lines, with IC50 values of 2.05μM, 5.74μM, 9.99μM and 17.54μM for TT, TPC1, BCPAP and K1 cells. The function of Y15 on this four cells through inhibition of FAK may due to increased detachment and necrosis, as well as decreased clonogenicity. Meanwhile, the distinct gene changes induced by Y15 from Defactinib may partially contribute to its synergism with Defactinib in medullary thyroid TT cells^[2].
作用机制Y15 can be docked into the structural pocket of FAK containing Y397 site.^[1]
动物研究
剂量
Mice^[3]: min = 30 mg/kg, max = 200 mg/kg

给药途径
i.p., p.o.

毒性数据 (半致死量)
MTD (sigal-dose) = 200 mg/kg, p.o.
MTD (multi-dose)= 100 mg/kg, p.o.^[3]
临床研究

动物研究
剂量	Mice^[3]: min = 30 mg/kg, max = 200 mg/kg
给药途径	i.p., p.o.
毒性数据 (半致死量)	MTD (sigal-dose) = 200 mg/kg, p.o. MTD (multi-dose)= 100 mg/kg, p.o.^[3]

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00289757	Hepatitis A	Phase 4	Completed	-	Belgium ... more >> GSK Investigational Site Wilrijk, Belgium, 2610 Collapse <<
NCT00289770	-	-	Completed	-	-
NCT00289757	-	-	Completed	-	-

更多
参考文献

[1] Hochwald SN, Nyberg C, et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle. 2009 Aug;8(15):2435-43. Epub 2009 Aug 1.
[2] O'Brien S, Golubovskaya VM, et al. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59.
[3] Golubovskaya V, Curtin L, et al. In vivo toxicity, metabolism and pharmacokinetic properties of FAK inhibitor 14 or Y15 (1, 2, 4, 5-benzenetetramine tetrahydrochloride). Arch Toxicol. 2015;89(7):1095-101.

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
- 3.5210 mL
- 17.6050 mL
- 35.2100 mL
- 5 mM
- 0.7042 mL
- 3.5210 mL
- 7.0420 mL
- 10 mM
- 0.3521 mL
- 1.7605 mL
- 3.5210 mL

技术信息

CAS号

4506-66-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C6H14Cl4N4

运输

蓝冰

分子量

284.01

别名

FAK Inhibitor 14;FAK Inhibitor Y15;Focal Adhesion Kinase Inhibitor 14;NSC 667249;NSC 677249

溶解度

DMSO	360.0 mg/mL (1267.5 mM)
Water	insoluble

动物实验配方

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NCT00289757	Hepatitis A	Phase 4	Completed	-	Belgium ... more >> GSK Investigational Site Wilrijk, Belgium, 2610 Collapse <<
NCT00289770	-	-	Completed	-	-
NCT00289757	-	-	Completed	-	-
NCT00289770	Hepatitis B H... more >>epatitis A Collapse <<	Phase 3	Completed	-	Belgium ... more >> GSK Investigational Site Wilrijk, Belgium, 2610 Collapse <<
NCT00289718	Hepatitis B H... more >>epatitis A Collapse <<	Phase 3	Completed	-	Belgium ... more >> GSK Investigational Site Gent, Belgium, 9000 Collapse <<
NCT00289718	-	-	Completed	-	-
NCT02037230	Adenocarcinoma of the Pancreas	Phase 1 Phase 2	Active, not recruiting	January 2022	United States, Michigan ... more >> University of Michigan Hospital Ann Arbor, Michigan, United States, 48109 Collapse <<
NCT02543541	Cancer	Not Applicable	Active, not recruiting	December 2018	United States, Ohio ... more >> Case Comprehensive Cancer Center Cleveland, Ohio, United States, 44106 Collapse <<
NCT02666183	Advanced Cancer	Not Applicable	Recruiting	June 2019	United States, Ohio ... more >> University Hospitals Cleveland Medical Center, Case Comprehensive Cancer Center Recruiting Cleveland, Ohio, United States, 44106 Contact: Sara Douglas, RN, PhD 216-368-0702 sld4@case.edu Principal Investigator: Sara Douglas, RN, PhD Collapse <<

Benzene-1,2,4,5-tetraamine tetrahydrochloride Catalog No. CSN17077

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