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AMD 3465

Catalog No. T14208 CAS 185991-24-6

Synonyms: GENZ-644494

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells.

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AMD 3465, CAS 185991-24-6

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Description	AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells.
Targets&IC50	HIV-2 (ROD):12.3 nM （in MT-4 cells), X4 HIV-1 (HE):9.8 nM （in MT-4 cells), X4 HIV-1 (RF):7.4 nM （in MT-4 cells), X4 HIV-1 (IIIB):12.3 nM （in MT-4 cells), 12G5 mAb-CXCR4:0.75 nM （in SupT1 cells), CXCL12 (AF647)-CXCR4:18 nM （in SupT1 cells), X4 HIV-1 (NL4.3):6.1 nM （in MT-4 cells), X4 HIV-1 (NL4.3AMD3100):2822 nM （in MT-4 cells), HIV-2 (EHO):12.3 nM （in MT-4 cells)
In vitro	AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells and it is cytotoxic to the X4 HIV-1 strains IIIB, NL4.3, RF and HE with an IC50 ranging from 6 to 12 nM. 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 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 of 17 nM. However, it 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. The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM[1].
In vivo	AMD 3465, administered subcutaneously at a dosage of 2.5 mg/kg/day for five weeks, significantly inhibits the growth of U87 glioblastoma multiforme (GBM) and Daoy xenograft tumors.

Synonyms	GENZ-644494
Molecular Weight	410.6
Formula	C24H38N6
CAS No.	185991-24-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61. 2. Yang L, et al. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Res. 2007 Jan 15;67(2):651-8.

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Keywords

AMD 3465 185991-24-6 Microbiology/Virology Proteases/Proteasome HIV Protease AMD3465 GENZ 644494 GENZ644494 AMD-3465 GENZ-644494 inhibitor inhibit

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