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• 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

• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *