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S81023

Bafetinib (INNO-406)

MedMol 96%
  • 英文名:
  • Bafetinib (INNO-406)
  • 别名:
  • NS-187;巴非替尼;N-[3-([4,5'-联嘧啶]-2-基氨基)-4-甲基苯基]-4-[[(3S)-3-(二甲基氨基)-1-吡咯烷基]甲基]-3-(三氟甲基)苯甲酰胺
  • CAS号:
  • 859212-16-1
  • 分子式:
  • C30H31F3N8O
  • 分子量:
  • 576.62
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
MedMol S81023-5mg 96% ¥325.00元 6 - - - EA 加入购物车
MedMol S81023-10mg 96% ¥510.00元 6 - - - EA 加入购物车
MedMol S81023-25mg 96% ¥722.50元 4 - - - EA 加入购物车
源叶(MedMol) S81023-100mg 96% ¥1785.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 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
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