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Bafetinib (INNO-406) 是一种特异性双重 Bcr-Abl/Lyn 抑制剂,IC50值为5.8和19 nM。
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Bafetinib (INNO-406) 是一种特异性双重 Bcr-Abl/Lyn 抑制剂,IC50值为5.8和19 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 278 | 现货 | |
2 mg | ¥ 392 | 现货 | |
5 mg | ¥ 622 | 现货 | |
10 mg | ¥ 977 | 现货 | |
25 mg | ¥ 1,530 | 现货 | |
50 mg | ¥ 1,930 | 5日内发货 | |
100 mg | ¥ 3,730 | 5日内发货 | |
200 mg | ¥ 5,330 | 5日内发货 | |
500 mg | ¥ 7,880 | 5日内发货 | |
1 mL x 10 mM (in DMSO) | ¥ 789 | 现货 |
产品描述 | Bafetinib (INNO-406) (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. |
靶点活性 | Lyn:19 nM, Abl:5.8 nM |
体外活性 | Bafetinib通过阻断WT Bcr-Abl自磷酸化及其下游激酶活性,对K562和293T细胞的IC50分别为11 nM和22 nM,有效抑制包括K562、KU812和BaF3/wt在内的Bcr-Abl阳性细胞系的生长,对Bcr-Abl阴性的U937细胞系增殖无影响。此外,Bafetinib对Bcr-Abl点突变细胞系(例如BaF3/E255K细胞)展示了剂量依赖的抗增殖效果。[1] 在Bcr-Abl阳性白血病细胞系中,Bafetinib通过阻断Bcr-Abl的磷酸化,诱导包括半胱天冬酶介导和非半胱天冬酶依赖的细胞死亡。[2] |
体内活性 | 在Bcr-Abl阳性的KU812小鼠模型中,Bafetinib(0.2 mg/kg/天)显著抑制肿瘤生长,在20 mg/kg/天的剂量下能完全抑制肿瘤生长,并且没有不良反应。对于Balb/c小鼠,Bafetinib的最大耐受剂量为200 mg/kg/d,生物可利用度(BA)值为32%。[1] 在携带Ba/F3/wt bcr-ablGFP、Ba/F3/Q252H或Ba/F3/M351T细胞的中枢神经系统(CNS)白血病模型中,Bafetinib(60 mg/kg)和环孢霉素A(CsA)(50 mg/kg)的组合治疗比单独使用Bafetinib或CsA更显著地抑制了大脑中白血病的生长。[3] |
激酶实验 | Kinase assay : Bcr-Abl kinase assays are 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 is used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn are carried out with an enzyme-linked immunosorbent assay (ELISA) kit. The inhibitory effects of NS-187 against 79 tyrosine kinases are tested with KinaseProfiler. |
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) |
别名 | 巴氟替尼, NS-187, INNO-406 |
分子量 | 576.62 |
分子式 | C30H31F3N8O |
CAS No. | 859212-16-1 |
Smiles | CN(C)[C@H]1CCN(Cc2ccc(cc2C(F)(F)F)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cncnc3)c2)C1 |
密度 | 1.36 g/cm3 |
存储 | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 93 mg/mL (161.3 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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