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• 產(chǎn)品描述： Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) 是一種 CXCR4 的拮抗劑，IC50值約為1 nM。BL-8040 通過改變的miR-15a/16-1的表達(dá)，下調(diào) ERK、BCL-2、MCL-1 和 cyclin-D1，誘導(dǎo)AML胚的凋亡

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

• 體外研究：
  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

• 體內(nèi)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

• 細(xì)胞實(shí)驗(yàn)： 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

• 動(dòng)物實(shí)驗(yàn)： Animal Models: female NOD scid gamma (NSG) mice (7-9 weeks old) Dosages: 400 μg/mouse Administration: SC

• 參考文獻(xiàn)：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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