Bosutinib hydrate
(Synonyms: SKI-606 hydrate) 目录号 : GC68796Bosutinib (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。
Cas No.:918639-08-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).
Bosutinib (drate) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively[1].
Bosutinib (drate) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2].
Cell Proliferation Assay[2]
| Cell Line: | The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84) |
| Concentration: | 0.1 μmol/L |
| Incubation Time: | 72 h |
| Result: | Inhibited several human CML derived cell lines with IC50 values ranging from 1 to 20 nmol/L. |
Bosutinib (drate) (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (drate) (150 mg/kg; once daily, 5 days weekly) has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2].
| Animal Model: | KU812CM L xenograft model[2] |
| Dosage: | 75 mg/kg twice daily or 150 mg/kg once daily |
| Administration: | Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) |
| Result: | Had the therapeutic activity and produced a dose- and schedule-dependent weight loss. |
| Animal Model: | Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2] |
| Dosage: | 150 mg/kg |
| Administration: | Bosutinib (150 mg/kg; once daily, 5 days weekly) |
| Result: | Decreased the rate of tumor growth and prolonged event-free survival of mice. |
[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.
| Cas No. | 918639-08-4 | SDF | Download SDF |
| 别名 | SKI-606 hydrate | ||
| 分子式 | C26H31Cl2N5O4 | 分子量 | 548.46 |
| 溶解度 | 储存条件 | 4°C, protect from light | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8233 mL | 9.1164 mL | 18.2329 mL |
| 5 mM | 0.3647 mL | 1.8233 mL | 3.6466 mL |
| 10 mM | 0.1823 mL | 0.9116 mL | 1.8233 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。