eCF506

An inhibitor of Src kinases

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库存: 现货

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5mg

￥1287.00

1030.00

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25mg

￥4175.00

3340.00

- +
50mg

￥6300.00

5040.00

- +
100mg

￥10587.00

8470.00

- +

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货号: ajce49892
CAS: 1914078-41-3
别名:
分子式: C26H38N8O3
分子量: 510.63
纯度: >98%
溶解度: DMSO : 62.5 mg/mL (122.40 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

eCF506 is an inhibitor of Src kinases (IC₅₀s = <0.5, 2.1, <0.5 nM for Src, Fyn, and Yes, respectively).¹ It is selective for Src kinases over Abl (IC₅₀ = 479 nM), as well as KIT, mTOR, PDGFRα, and RET (IC₅₀s = >100 ?M for all). eCF506 completely inhibits phosphorylation of Src and FAK, a downstream Src substrate, in MCF-7 and MDA-MB-231 cells when used at a concentration of 100 nM. It also inhibits proliferation of MCF-7 cells (EC₅₀ = 9 nM) and induces apoptosis. eCF506 (50 mg/kg per day) reduces levels of activated Src kinase in tumor tissue in an HCT116 mouse xenograft model.

1.Fraser, C., Dawson, J.C., Dowling, R., et al.Rapid discovery and structure-activity relationships of pyrazolopyrimidines that potently suppress breast cancer cell growth via SRC kinase inhibition with exceptional selectivity over ABL kinaseJ. Med. Chem.59(10)4697-4710(2016)

Protocol

Cell experiment:

MDA-MB-231 cells are treated with eCF506 or dasatinib (10 nM), and cell migration compared with untreated cell control (DMSO, 0.1%, v/v) at 6, 12, and 24 h. Cells are imaged and analyzed using an IncuCyte-ZOOM microscope with integrated scratch-wound migration software module[1].

Animal experiment:

Mice[1]In vivo PD study is performed in a xenograft model of HCT116 cells in mice. HCT116 cells are injected subcutaneously, and tumors are allowed to grow up to 3-mm in diameter. Subsequently, mice are dosed daily for 3 d with eCF506 (50 mg/kg, in nanopure water) or vehicle (nanopure water) by oral gavage and culled 3 h after the last dose (n=4). Tumors are excised, fixed, and sections labeled for phospho-SRCY416 and stained with hematoxylin[1].

参考文献:

[1]. Fraser C, et al. Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710.