Bafetinib
(Synonyms: 巴氟替尼; INNO-406; NS-187) 目录号 : GC35462
A Bcr-Abl inhibitor
Cas No.:859212-16-1
Sample solution is provided at 25 µL, 10mM.
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Bcr-Abl, a fusion protein with deregulated tyrosine kinase activity, is highly expressed in chronic myelogenous leukemia (CML). Bafetinib is a rationally developed tyrosine kinase inhibitor based on the chemical structure of imatinib , with modifications added to improve binding and potency against Bcr-Abl kinase (IC50 = 5.8 nM).1 It is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo.1 Bafetinib inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation and also targets the Src family kinase Lyn (IC50 = 19 nM), which has been associated with resistance to imatinib in CML.1
1.Kimura, S., Naito, H., Segawa, H., et al.NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemiaBlood106(12)3948-3954(2005)
| Kinase experiment [1]: | |
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Kinase assays |
Bcr-Abl kinase assays were performed in 25 μL of reaction mixture containing 250 μM peptide substrate, 740 Bq/μL [γ-33P]ATP, and 20 μM cold adenosine triphosphate (ATP) by using the SignaTECT protein tyrosine kinase assay system. Each Bcr-Abl kinase was used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn were carried out with an enzyme-linked immunosorbent assay (ELISA) kit from Carna Biosciences. |
| Cell experiment [1]: | |
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Cell lines |
K562, BaF3/wt and KU812 cell lines |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. 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 |
0-10 μM for 3 days |
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Applications |
Bafetinib could suppress the growth of the Bcr-Abl–positive cell lines K562, KU812, and BaF3/wt. |
| Animal experiment [1]: | |
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Animal models |
Bcr-Abl–positive KU812 mouse model |
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Dosage form |
0.2 mg/kg/d and 20 mg/kg/d orally twice a day for 26 consecutive days |
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Application |
Bafetinib suppressed the growth of Bcr-Abl–bearing tumors (KU812) and markedly extends the survival of mice bearing such tumors. |
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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]. Kimura S, Naito H, Segawa H, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood, 2005, 106(12): 3948-3954. |
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| Cas No. | 859212-16-1 | SDF | |
| 别名 | 巴氟替尼; INNO-406; NS-187 | ||
| 化学名 | (S)-N-(3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-3-(trifluoromethyl)benzamide | ||
| Canonical SMILES | O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CN=CN=C3)=N2)=C1)C4=CC=C(CN5C[C@@H](N(C)C)CC5)C(C(F)(F)F)=C4 | ||
| 分子式 | C30H31F3N8O | 分子量 | 576.62 |
| 溶解度 | DMSO: ≥ 42 mg/mL (72.84 mM) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7342 mL | 8.6712 mL | 17.3424 mL |
| 5 mM | 0.3468 mL | 1.7342 mL | 3.4685 mL |
| 10 mM | 0.1734 mL | 0.8671 mL | 1.7342 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet