|BKT140游离态|CsnPharm

CAS No.: 664334-36-5

Motixafortide/莫替昔福特（三氟乙酸盐） Catalog No. CSN18996

Synonyms: BKT140 (4-fluorobenzoyl);BL-8040;TF14016

BKT140 is a CXCR4 antagonist with an IC50 value of ~1 nM.

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技术信息

生物活性

描述The chemokine receptor CXCR4 and its ligand CXCL12 are involved in the progression and dissemination of a diverse number of solid and hematological malignancies. Binding CXCL12 to CXCR4 activates a variety of intracellular signal transduction pathways that regulate cell chemotaxis, adhesion, survival, proliferation, and apoptosis^[3]. CXCR4 plays an important role in the retention of stem cells within the bone marrow^[4]. BKT140 (4F-benzoyl-TN14003), a novel CXCR4 antagonist, binds and inhibits the CXCR4 chemokine receptor with high affinity, showing an IC₅₀ of ∼1 nM. Moreover, BKT140 hinders the cell migration stimulated by CXCL12 within IC₅₀ values of 0.5 to 2.5 nM, suggesting a high mobilization capacity^[4]. BKT140 displays selective toxicity toward AML and MM cells. Treatment with BKT140 can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. BKT140 specifically triggers CXCR4-dependent cell death and stimulates apoptotic cell death in leukemia and MM cells^[3]. Subcutaneous injections of BKT140 significantly reduce, in a dose-dependent manner, the growth of human acute myeloid leukemia and multiple myeloma xenografts. Tumors from animals treated with Motixafortide (BKT140) are smaller in size and weights and had larger necrotic areas and higher apoptotic scores^[3]. BKT140 was well tolerated at all concentrations, and none of the patients developed grade 3 and 4 toxicity. A single administration of BKT140 at the highest dose, 0.9 mg/kg, resulted in a robust mobilization and collection of CD34 (+) cells (20.6 ± 6.9 × 10⁶/kg), which were obtained through a single apheresis^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01010880	Multiple Myeloma	Phase 1 Phase 2	Completed	-	Israel ... more >> Department of Hematology and Bone Marrow Transplantation,Rambam Medical Center Haifa, Israel, 31096 Chaim Sheba Medical Center,Tel-Hashomer Ramat Gan, Israel, 52621 Collapse <<

参考文献

[1] Peled A, Abraham M, et al. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cells in patients with multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79.
[2] Beider K, Begin M, et al. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011 Mar;39(3):282-92.
[3] Beider K, Begin M, Abraham M, Wald H, Weiss ID, Wald O, Pikarsky E, Zeira E, Eizenberg O, Galun E, Hardan I, Engelhard D, Nagler A, Peled A. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011 Mar;39(3):282-92. doi: 10.1016/j.exphem.2010.11.010. Epub 2010 Dec 5. PMID: 21138752.
[4] Peled A, Abraham M, Avivi I, Rowe JM, Beider K, Wald H, Tiomkin L, Ribakovsky L, Riback Y, Ramati Y, Aviel S, Galun E, Shaw HL, Eizenberg O, Hardan I, Shimoni A, Nagler A. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cells in patients with multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79. doi: 10.1158/1078-0432.CCR-13-1302. Epub 2013 Nov 18. PMID: 24246358.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.4631 mL
- 2.3153 mL
- 4.6307 mL
- 5 mM
- 0.0926 mL
- 0.4631 mL
- 0.9261 mL
- 10 mM
- 0.0463 mL
- 0.2315 mL
- 0.4631 mL

技术信息

CAS号	664334-36-5	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C97H144FN33O19S2	运输	蓝冰
分子量	2159.52	别名	BKT140 (4-fluorobenzoyl);BL-8040;TF14016;4F-Benzoyl-TN 14003;BKT-140;BL-8040. TN-14003

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Motixafortide/莫替昔福特 （三氟乙酸盐） Catalog No. CSN18996

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Motixafortide/莫替昔福特（三氟乙酸盐） Catalog No. CSN18996