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CAS No.: 2309699-17-8

Mavorixafor 3HCl Catalog No. CSN24435

Synonyms: AMD-070 trihydrochloride;Mavorixafor 3HCl;AMD-11070 3HCl

AMD-070 is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.

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技术信息

生物活性

描述The G protein-coupled protein receptor C-X-C chemokine receptor 4 (CXCR4) is an attractive target for cancer diagnosis and treatment, as it is overexpressed in many solid and hematologic cancers^[1]. Mavorixafor 3HCl represents the first small molecule orally bioavailable CXCR4 antagonist that was developed for the treatment of HIV-1 infection. It is a potent, selective and orally available CXCR4 antagonist with an IC₅₀ value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC₅₀ of 2 and 26 nM, respectively, while remaining noncytotoxic to cells at concentrations exceeding 23 μM^[2]. Mavorixafor 3HCl at 6.6 µM significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells^[3]. The pharmacokinetics of mavorixafor 3HCl was evaluated in rat and dog, and good oral bioavailability was observed in both species^[2]. Mavorixafor 3HCl (2 mg/kg, p.o.) significantly reduced the number of metastatic lung nodules in mice, and lowers the expression of human Alu DNA in mice, without body weight loss^[3].
参考文献

[1] Walenkamp AME, Lapa C, Herrmann K, Wester HJ. CXCR4 Ligands: The Next Big Hit? J Nucl Med. 2017 Sep;58(Suppl 2):77S-82S. doi: 10.2967/jnumed.116.186874. PMID: 28864616.
[2] Skerlj RT, Bridger GJ, Kaller A, McEachern EJ, Crawford JB, Zhou Y, Atsma B, Langille J, Nan S, Veale D, Wilson T, Harwig C, Hatse S, Princen K, De Clercq E, Schols D. Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication. J Med Chem. 2010 Apr 22;53(8):3376-88. doi: 10.1021/jm100073m. PMID: 20297846.
[3] Uchida D, Kuribayashi N, Kinouchi M, Sawatani Y, Shimura M, Mori T, Hasegawa T, Miyamoto Y, Kawamata H. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells. Oncol Rep. 2018 Jul;40(1):303-308. doi: 10.3892/or.2018.6400. Epub 2018 Apr 25. PMID: 29749473.

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
- 2.1793 mL
- 10.8967 mL
- 21.7934 mL
- 5 mM
- 0.4359 mL
- 2.1793 mL
- 4.3587 mL
- 10 mM
- 0.2179 mL
- 1.0897 mL
- 2.1793 mL

技术信息

CAS号	2309699-17-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C21H30Cl3N5	运输	蓝冰
分子量	458.86	别名	AMD-070 trihydrochloride;Mavorixafor 3HCl;AMD-11070 3HCl;X4P 001 3HCl

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