Saracatinib

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Chemical Structure| 379231-04-6 同义名 : AZD0530
CAS号 : 379231-04-6
货号 : A154045
分子式 : C27H32ClN5O5
纯度 : 99%+
分子量 : 542.03
MDL号 : MFCD09832698
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(92.25 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • EGFR/ErbB1

    EGFR (L861Q), IC50:4 nM

    EGFR, IC50:5 nM

  • Fyn

    Fyn, IC50:10 nM

  • Src

    c-Src, IC50:2.7 nM

  • Lck

    LCK, IC50:<4 nM

  • Lyn

    Lyn, IC50:5 nM
描述 Saracatinib is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck and is less active for Abl and EGFR (L858R and L861Q).
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
697 Growth Inhibition Assay IC50=13.2701 μM SANGER
A253 Growth Inhibition Assay IC50=35.7429 μM SANGER
A388 Growth Inhibition Assay IC50=5.63667 μM SANGER
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
NCT01144481 - Completed - Canada, Ontario ... 展开 >> University Health Network Toronto, Ontario, Canada, M5G 2C4 收起 <<
NCT00265876 Pancreatic Cancer Phase 1 Phase 2 Completed - Canada, British Columbia ... 展开 >> BCCA - Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Ottawa Health Research Institute - General Division Ottawa, Ontario, Canada, K1H 8L6 Algoma District Cancer Program Sault Ste. Marie, Ontario, Canada, P6B 0A8 Univ. Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT01000896 Cancer Non Sm... 展开 >>all Cell Lung Cancer Epithelial Ovarian Cancer 收起 << Phase 1 Withdrawn(AstraZeneca has disc... 展开 >>ontinued the development of AZD0530. No new AstraZeneca-sponsored clinical studies will be initiated..) 收起 << March 2011 Japan ... 展开 >> Research Site Matsuyama, Ehime, Japan Research Site Fukuoka, Japan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.22mL

1.84mL

0.92mL

18.45mL

3.69mL

1.84mL
参考文献

[1]Green TP, Fennell M, et al. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol. 2009 Jun;3(3):248-61.

[2]Chang YM, Bai L, et al. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene. 2008 Oct 23;27(49):6365-75.