产品说明书

Bosutinib

Print
Chemical Structure| 380843-75-4 同义名 : 伯舒替尼 (SKI-606) ;SKI-606
CAS号 : 380843-75-4
货号 : A730879
分子式 : C26H29Cl2N5O3
纯度 : 99%
分子量 : 530.45
MDL号 : MFCD07367846
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(84.83 mM)，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
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

生物活性
靶点

  • Src

    Src, IC50:1.2 nM
描述 Bosutinib is an orally active inhibitor of Src/Abl tyrosine kinases, with IC50 values of 1.2 nM and 1 nM, respectively[1]. Bosutinib is an active inhibitor of Bcr-Abl in various chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
23132-87 Growth Inhibition Assay IC50=15.8495 μM SANGER
5637 Growth Inhibition Assay IC50=1.13803 μM SANGER
647-V Growth Inhibition Assay IC50=29.7003 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
NCT02551718 Acute Leukemia of Ambiguous Li... 展开 >>neage Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia Refractory Adult Acute Lymphoblastic Leukemia Refractory Childhood Acute Lymphoblastic Leukemia 收起 << Not Applicable Recruiting - United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Pamela S. Becker    206-616-1589    pbecker@u.washington.edu    Principal Investigator: Pamela S. Becker 收起 <<
NCT03610971 Chronic Phase Chronic Myeloid ... 展开 >>Leukemia Chronic Myeloid Leukemia, Chronic Phase 收起 << Phase 2 Not yet recruiting January 2022 United States, Florida ... 展开 >> H. Lee Moffitt Cancer Center and Research Institute Not yet recruiting Tampa, Florida, United States, 33612 Contact: Anthony McLaughlin    813-745-5941    anthony.mclaughlin@moffitt.org    Contact: Kendra Sweet, M.D.    813-745-8986    kendra.sweet@moffitt.org    Principal Investigator: Kendra Sweet, M.D. 收起 <<
NCT03746054 Chronic Myeloid Leukemia (CML) Phase 3 Not yet recruiting March 2023 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.43mL

1.89mL

0.94mL

18.85mL

3.77mL

1.89mL
参考文献

[1]Jorge E Cortes, et al. Bosutinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: results from the BELA trial. J Clin Oncol. 2012 Oct 1;30(28):3486-92.

[2]Miriam Puttini, et al. In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. Cancer Res. 2006 Dec 1;66(23):11314-22.