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Bafetinib (INNO-406)

现货
Catalog No.
B1011
Bcr-Abl/Lyn酪氨酸激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
现货
5mg
¥ 750.00
现货
10mg
¥ 1,390.00
现货
25mg
¥ 2,430.00
现货
100mg
¥ 4,880.00
现货

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Background

Bafetinib is a potent and selective dual inhibitor of Bcr-Abl/Lyn tyrosine kinase with IC50 values of 5.8nM and 19nM, respectively [1].

Bafetinib is a specific dual Abl-Lyn inhibitor. For 79 other tyrosine kinases, 0.1μM bafetinib can inhibit 4 of these enzymes including Abl, Abl-related gene, Fyn and Lyn. Bafetinib can block the autophosphorylation of Bcr-Abl. In K562 and 293T cells transfected with wt Bcr-Abl, bafetinib shows inhibition with IC50 values of 11nM and 22nM, respectively. In the in vitro kinase assays, bafetinib shows inhibition of a variety of Abl kinase mutants such as M244V, G250E, Y253F and F317L. It has no effect on T315I in vitro. Bafetinib also suppresses the growth of Bcr-Abl–positive leukemic cell lines including K562, KU812 and BaF3/wt. The BaF3/E255K cells are also sensitive towards bafetinib. Moreover, bafetinib is highly potent to inhibit tumor growth in murine tumor models [1].

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.

文献引用

1.Gabriella R. Sterne. "Signaling mechanisms of Down syndrome cell adhesion molecule in presynaptic arbor size control." University of Michigan.2016.
2.Sterne, Gabriella R., Jung Hwan Kim, and Bing Ye. "Dysregulated Dscam levels act through Abelson tyrosine kinase to enlarge presynaptic arbors." eLife 4 (2015): e05196. PMID:25988807

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt576.62
Cas No.887650-05-7; 859212-16-1
FormulaC30H31F3N8O
Solubility≥57.7mg/mL in DMSO
Chemical Name4-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]methyl]-N-[4-methyl-3-[(5-pyrimidin-5-ylpyrimidin-2-yl)amino]phenyl]-3-(trifluoromethyl)benzamide
SDFDownload SDF
Canonical SMILESCC1=C(C=C(C=C1)NC(=O)C2=CC(=C(C=C2)CN3CCC(C3)N(C)C)C(F)(F)F)NC4=NC=C(C=N4)C5=CN=CN=C5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

酶学实验 [1]:

激酶实验

通过使用SignaTECT蛋白酪氨酸激酶实验系统,Bcr-Abl激酶实验是在25微升反应混合物中进行:250微摩尔多肽底物,740Bq/微升[γ-33P]ATP,20微摩尔冷ATP。Bcr-Abl激酶浓度为10纳摩尔。Abl、Src和Lyn激酶实验运用ELISA试剂盒进行。

细胞实验 [1]:

细胞系

K562,BaF3/wt和KU812细胞系

溶解方法

在DMSO中的溶解度> 10 mM。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0-10 μM孵育3天

应用

Bafetinib能够抑制Bcr-Abl阳性细胞系(K562,BaF3/wt和KU812)生长。

动物实验 [1]:

动物模型

Bcr-Abl阳性KU812荷瘤裸鼠

剂量

0.2和20毫克/千克每天;每天两次口服给药;持续26天

应用

Bafetinib可抑制Bcr-Abl阳性荷瘤小鼠(KU812)的肿瘤生长,也能显著延长生存期。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

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.

生物活性

Description Bafetinib(INNO-406)是一种口服生物可利用的Bcr-Abl和Lyn激酶双重抑制剂,IC50值分别为5.8 nM/19 nM。
靶点 Abl Lyn        
IC50 5.8 nM 19 nM        

质量控制

化学结构

Bafetinib

相关生物数据

Bafetinib

相关生物数据

Bafetinib