Radotinib(IY-5511)
(Synonyms: 拉多替尼) 目录号 : GC11140
A selective Bcr-Abl tyrosine kinase inhibitor
Cas No.:926037-48-1
Sample solution is provided at 25 µL, 10mM.
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Radotinib(IY-5511) is a novel and selective Bcl-Abl tyrosine kinase inhibitor. [1]
Bcl-Abl is a constitutively activated chimeric tyrosine kinase which is the genetic abnormality expressed in patient with CML (chronic myeloid leukemia).
In vitro, radotinib couples to Bcr-Abl and reduce the phosphorylation of Bcr-Abl target protein CrkL. The pre-clinical studies shows superiority of radotinib to imatinib in both wild-type and mutant BCR-ABL1 positive CML cell lines. [1]
In a phase I clinical trial, dose up to 1000 mg/day of radotinib exhibits no dose-limiting toxicities. Phase II study proves radotinib to be an effective and well tolerated in chronic phase-chronic myeloid leukemia patients with resistance and/or intolerance to Bcr-Abl1 tyrosine kinase inhibitors. [1]
Reference:
1. Kim SH, Menon H, Jootar S et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Haematologica. 2014 Jul;99(7):1191-6.
| Cell experiment [1]: | |
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Cell lines |
Bone marrow cells (BMCs) from patients with AML |
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Preparation method |
The solubility of this compound in DMSO is > 26.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1, 10, and 100 µM, 72 h, 37 ℃ |
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Applications |
Radotinib is an inhibitor of BCR-ABL1 tyrosine kinase and has been approved for the second-line treatment of chronic myeloid leukemia. In BMCs from patients with AML, radotinib increased cleaved caspase-3, caspase-7, and caspase-9 levels, resulting in increasing apoptosis. Radotinib also induced G0/G1 phase arrest and inhibited proliferating of BMCs from patients with AML. |
| Clinical experiment [2]: | |
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Clinical samples |
Patients at least 18 years of age with Philadelphia chromosome-positive chronic phase-CML with resistance and/or intolerance to imatinib. |
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Dosage form |
400 mg, twice daily |
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Application |
Patients’ response to radotinib is comparable to other 2nd-generation tyrosine kinase inhibitors. Radotinib is well tolerated and effective in chronic phase-chronic myeloid leukemia patients with resistance and/or intolerance to imatinib. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Heo S K, Noh E K, Gwon G D, et al. Radotinib inhibits acute myeloid leukemia cell proliferation via induction of mitochondrial-dependent apoptosis and CDK inhibitors[J]. European journal of pharmacology, 2016, 789: 280-290. [2]. Kim S H, Menon H, Jootar S, et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors[J]. Haematologica, 2014: haematol. 2013.096776. | |
| Cas No. | 926037-48-1 | SDF | |
| 别名 | 拉多替尼 | ||
| 化学名 | (Z)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-(pyrazin-2-yl)pyrimidin-2-yl)amino)benzimidic acid | ||
| Canonical SMILES | CC1=C(NC2=NC=CC(C3=CN=CC=N3)=N2)C=C(/C(O)=N/C4=CC(N(C=N5)C=C5C)=CC(C(F)(F)F)=C4)C=C1 | ||
| 分子式 | C27H21F3N8O | 分子量 | 530.5 |
| 溶解度 | ≥ 26.55mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.885 mL | 9.4251 mL | 18.8501 mL |
| 5 mM | 0.377 mL | 1.885 mL | 3.77 mL |
| 10 mM | 0.1885 mL | 0.9425 mL | 1.885 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet