同义名 :	AMD-070 trihydrochloride; Mavorixafor trihydrochloride; AMD-11070 trihydrochloride
	CAS号 :	2309699-17-8
	货号 :	A1166471
	分子式 :	C21H30Cl3N5
	纯度 :	98%
	分子量 :	458.86
	MDL号 :	N/A
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.18mL 0.44mL 0.22mL	10.90mL 2.18mL 1.09mL	21.79mL 4.36mL 2.18mL

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.