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CAS No.: 1391712-60-9

CEP-37440 Catalog No. CSN16907

Synonyms: CEP-37440

CEP-37440 is a potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM (ALK cellular IC50 in 75% human plasma).

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400-920-2911

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技术信息

生物活性

描述Focal adhesion kinase 1 (FAK1) is a nonreceptor tyrosine kinase that binds epidermal growth factor receptor (EGFR), vascular epidermal growth factor receptor (VEGFR), p53 and other molecules that are critical for tumor growth and progression. CEP-37440 is a potent ATP- competitive and orally active inhibitor of FAK1 with enzymatic IC50 value of 2.0 nM and cellular IC50 value of 82 nM. CEP-37440 also inhibits anaplastic lymphoma kinase (ALK) with enzymatic IC50 value of 3.1 nM and cellular IC50 of 22 nM^[1]. In vitro, CEP-37440 suppressed proliferation of inflammatory breast cancer (IBC) cell lines FC-IBC02, KPL4, SUM190 and MDA-IBC03 with GI50 values of 91 nM, 900 nM, 890 nM and 1860 nM, respectively. CEP-37440 also suppressed proliferation of breast cancer (BC) cell lines MDA-MB-231, MDA-MB-468 and normal like breast epithelial cell lines MCF-12A, MCA-10A with GI50 values of 1930 nM, 1275 nM, 1516 nM and 1700 nM, respectively. CEP-37440 at concentration of 1000 nM decreased phosphor-FAK1 in IBC cell lines FC-IBC02, SUM190, and KPL4 cells after 48h of treatment. Expression array analyses in FC-IBC02 cells showed that CEP-37440 affects the expression of genes related to apoptosis, interferon signaling, and cytokines. In vivo, oral administration of CEP-37440 at 55 mg/kg twice a day for 7 weeks inhibited the SUM190, FC-IBC02, and SUM149 breast tumor xenografts in mice with the tumor growth inhibition (TGI) of 79.7%, 33% and 23%, respectively. In addition, CEP37440 inhibited the brain metastasis in the FC-IBC02 breast xenografts mice^[2]. CEP-37440 was undergoing clinical development in phase I in patients with advanced or metastatic solid tumours but no preliminary data are available^[3].
作用机制CEP-37440 inhibits the activation of FAK1 by inhibiting the phosphorylation Tyr397 of FAK1^[2].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01922752	Solid Tumors	Phase 1	Completed	-	United States, Illinois ... more >> Teva Investigational Site 10689 Chicago, Illinois, United States United States, Pennsylvania Teva Investigational Site 10687 Philadelphia, Pennsylvania, United States United States, Texas Teva Investigational Site 10686 San Antonio, Texas, United States Collapse <<

参考文献

[1] Ott G R, Cheng M, Learn K S, et al. Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). Journal of Medicinal Chemistry, 2016, 59(16): 7478-7496
[2] Salem I, Alsalahi M, Chervoneva I, et al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and In vivo on inflammatory breast cancer cells. Breast Cancer Research, 2016, 18(1): 37-37
[3] Sullivan I, Planchard D. ALK inhibitors in non-small cell lung cancer: the latest evidence and developments.Therapeutic Advances in Medical Oncology, 2016, 8(1): 32-47

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
- 1.7238 mL
- 8.6189 mL
- 17.2378 mL
- 5 mM
- 0.3448 mL
- 1.7238 mL
- 3.4476 mL
- 10 mM
- 0.1724 mL
- 0.8619 mL
- 1.7238 mL

技术信息

CAS号

1391712-60-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H38ClN7O3

运输

蓝冰

分子量

580.12

别名

CEP-37440

溶解度

DMSO	41.0 mg/mL (70.7 mM)

动物实验配方

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