货号	规格	价格	上海	北京	珠海	重庆	武汉
S86140-1mg	≥99%	￥850.00 S86140-1mg ￥850.00 3-5天	0 货期：3-5天	-	-	-	-
S86140-5mg	≥99%	￥1520.00 S86140-5mg ￥1520.00 3-5天	0 货期：3-5天	-	-	-	-
S86140-10mg	≥99%	￥2550.00 S86140-10mg ￥2550.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S86140-1mg

≥99%

￥850.00

货期：3-5天

S86140-5mg

≥99%

￥1520.00

货期：3-5天

S86140-10mg

≥99%

￥2550.00

货期：3-5天

产品描述：

Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) 是一种 CXCR4 的拮抗剂，IC50值约为1 nM。BL-8040 通过改变的miR-15a/16-1的表达，下调 ERK、BCL-2、MCL-1 和 cyclin-D1，诱导AML胚的凋亡

靶点：

ERK; Bcl-2; MCL-1; cyclin-D1; CXCR4(Cell-free assay):1 nM;CXCR

体外研究：

Treatment with BL-8040 induces the robust mobilization of AML blasts from the BM. In addition, AML cells exposed to BL-8040 undergoes differentiation. BL-8040 induces the apoptosis of AML cells in vitro. This apoptosis is mediated by the up-regulation of miR-15a/miR-16-1, resulting in down-regulation of the target genes BCL-2, MCL-1 and cyclin-D1. Overexpression of miR-15a/miR-16-1 directly induces leukemic cell death. BL-8040-induced apoptosis is also mediated by the inhibition of survival signals via the AKT/ERK pathways

体内研究：

BL-8040 induces the apoptosis of AML cells in vivo. Treatment with a BCL-2 inhibitor induces apoptosis and acts together with BL-8040 to enhance cell death. BL-8040 also synergizes with FLT3 inhibitors to induce AML cell death. Importantly, this combined treatment prolongs the survival of tumor-bearing mice and reduces minimal residual disease in vivo

细胞实验：

Cell lines: The leukemic cell lines (MV4-11, THP-1, U937, HL-60) Concentrations: 0.1 μM, 1 μM, 10 μM, 20 μM Incubation Time: 24 h, 48 h Method: Cells are seeded in triplicate at 2×105 cells/well in a total volume of 250 μl in a 96-well plate in medium supplemented with 1% FCS RPMI medium for 24hr in the presence of BL-8040/AMD3100 (0.1, 1, 10 or 20μM) or ABT-199 (0.01, 0.1, 1 or 10μM). To test the combination of BL-8040 and ABT-199, cells are incubated for 24hr with BL-8040 (20μM) and ABT-199 (0.01, 0.1, 1 or 10μM). To test the combined effects of BL-8040 and AC220, cells are incubated for 48 hr with BL-8040 (20μM), AC220 (50nM) or a combination of the two. After incubation, cells are stained with propidium iodide (PI), and the percentage of dead cells (PI+ cells) in the culture is measured using a FACSCalibur machine

动物实验：

Animal Models: female NOD scid gamma (NSG) mice (7-9 weeks old) Dosages: 400 μg/mouse Administration: SC

参考文献：

1. M Abraham, et al. The CXCR4 inhibitor BL-8040 induces the apoptosis of AML blasts by downregulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression. Leukemia. 2017 Nov;31(11):2336-2346.

溶解性：

Soluble in H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	0.463 ml	2.315 ml	4.631 ml
5 mM	0.093 ml	0.463 ml	0.926 ml
10 mM	0.046 ml	0.232 ml	0.463 ml
50 mM	0.009 ml	0.046 ml	0.093 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。

参考文献

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