Bosutinib hydrate (Synonyms: SKI-606 hydrate)
目录号: PL01253 纯度: ≥99%
CAS No. :918639-08-4
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中文名称
Bosutinib hydrate
中文别名
博舒替尼一水化合物
英文名称
Bosutinib hydrate
英文别名
Bosutinib monohydrate;4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile,hydrate;bosutinib hydrate
Cas No.
918639-08-4
分子式
C26H31Cl2N5O4
分子量
548.46
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
Bosutinib (hydrate) 是一种口服Src/Abl酪氨酸激酶抑制剂,IC50分别为1.2 nM和1 nM。
生物活性
Bosutinib (hydrate) is an oral Src/Abl tyrosine kinase inhibito with IC 50 of 1.2 nM and 1 nM, respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).
体外研究(In Vitro)
Bosutinib (hydrate) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
Bosutinib (hydrate) (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (hydrate) (150 mg/kg; once daily, 5 days weekly) has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
ClinicalTrial
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.
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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