Bafetinib (INNO-406)

96.80%

Bafetinib (INNO-406)

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品牌：源叶(MedMol)

产品编号：S81023 一键复制产品信息

CAS号：859212-16-1

分子式：C₃₀H₃₁F₃N₈O

分子量：576.62

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

货号	规格	价格	上海	北京	珠海	重庆	武汉
S81023-5mg	96.80%	￥325.00 S81023-5mg ￥325.00 现货	6 6	-	-	-	-
S81023-10mg	96.80%	￥510.00 S81023-10mg ￥510.00 现货	6 6	-	-	-	-
S81023-25mg	96.80%	￥722.00 S81023-25mg ￥722.00 现货	4 4	-	-	-	-
S81023-100mg	≥96%	￥1958.00 S81023-100mg ￥1958.00 2-3天	0 货期：2-3天	-	-	-	-

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产品介绍参考文献质检证书(COA) 摩尔浓度计算器相关产品

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