AMD-070

Research use only, not for human use.

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay; displays no significant activity (IC50>10 uM) for a series of other closely GPCRs (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2); inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with IC50 of 2 nM and 26 nM, respectively, with noncytotoxic to cells (>23 uM); exhibits good PK profiles and excellent oral bioavailability; also inhibits CXCR4/SDF-1-mediated events in ALL cancer cells and transplant models.HIV Infection Phase 3 Clinical.

Mavorixafor (AMD-070) is a potent and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively. Mavorixafor (AMD-070) shows no effect on other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2). Mavorixafor (AMD-070) (6.6 μM) significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells.

Mavorixafor (AMD-070) (2 mg/kg, p.o.) significantly reduces the number of metastatic lung nodules in mice, and lowers the expression of human Alu DNA in mice, without body weight loss.

AMD-11070

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Infection

HIV Infection

558447-26-0

349.4726

C21H27N5

>98% (HPLC)

10 mM in DMSO

C1CC(C2=C(C1)C=CC=N2)N(CCCCN)CC3=NC4=CC=CC=C4N3

1,4-Butanediamine, N1-(1H-benzimidazol-2-ylmethyl)-N1-[(8S)-5,6,7,8-tetrahydro-8-quinolinyl]-

(-20℃)

With Ice Pack

≥ 2 years