AMD 3465 hexahydrobromide是一种CXCR4受体拮抗剂，具有潜在的抗癌和抗 HIV 活性。

AMD 3465 hexahydrobromide is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

AMD 3465 hexahydrobromide inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells.?AMD 3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 of 17 nM, but shows no effect on the intracellular calcium fluxes elicited by the CCR5 ligands RANTES, LD78β and MIP-1β in U87.CD4.CCR5 cells.?AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.?AMD3465 is cytotoxic to the X4 HIV-1 strains IIIB, NL4.3, RF and HE with an IC50 ranging from 6 to 12 nM.?The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM[1].?AMD 3465 inhibits CXCL-12-induced growth in U87 and Daoy cells.?AMD 3465 treatment stimulates the phosphorylation of Erk1/2 in U87 and Daoy cells[2].

AMD 3465 with 2.5 mg/kg/d, s.c. for 5 weeks significantly blocks the growth of U87 GBM and Daoy xenografts[2]

185991-07-5

C24H44Br6N6

896.082

GENZ-644494 (hexahydrobromide)

H2O:38 mg/mL (42.41 mM)
DMSO:50 mg/mL (55.80 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years