| 产品描述： | Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR. |
| 靶点： |
Autophagy；Bcr-Abl；Src;Others |
| 体内研究： |
In Bcr-Abl–positive KU812 mouse model, Bafetinib (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day. For Balb/c mice, Bafetinib shows maximal tolerated dose of 200 mg/kg/d and bioavailability value (BA) of 32%. [1] In a Central nervous system (CNS) leukemia model bearing Ba/F3/wt bcr-ablGFP, Ba/F3/Q252H, or Ba/F3/M351T cells, combination treatment of Bafetinib (60 mg/kg) and cyclosporine A (CsA) (50 mg/kg) leads to more significant inhibition of leukemia growth in the brain than either Bafetinib or CsA alone |
| 细胞实验： |
K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells are plated at 1 × 103 in 96-well plates, whereas KU812 and U937 cells are plated at 5 × 103 in 96-well plates. Cells are incubated with serial dilutions of Bafetinib for 3 days. Cell proliferation is measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Nacalai Tesque) assay, and the 50% inhibitory concentration (IC50) values are calculated by fitting the data to a logistic curve. (Only for Reference) |
| 参考文献： |
1.Kimura S, et al. Blood. 2005, 106(12), 3948-3954. 2.Jing Y, Dai X, Yang L, et al. STING couples with PI3K to regulate actin reorganization during BCR activation[J]. Science Advances. 2020, 6(17): eaax9455. 3.Kamitsuji Y, et al. Cell Death Differ. 2008, 15(11), 1712-2172. 4.Yokota A, et al. Blood. 2007, 109(1), 306-314. |
| 溶解性： |
Ethanol:<1 mg/mL DMSO:93 mg/mL (161.3 mM) H2O:<1 mg/mL |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.734 ml |
8.671 ml |
17.342 ml |
| 5 mM |
0.347 ml |
1.734 ml |
3.468 ml |
| 10 mM |
0.173 ml |
0.867 ml |
1.734 ml |
| 50 mM |
0.035 ml |
0.173 ml |
0.347 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京