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AMD 3465 hexahydrobromide

Catalog No. T7208 CAS 185991-07-5

Synonyms: GENZ-644494 (hexahydrobromide)

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

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AMD 3465 hexahydrobromide Chemical Structure

AMD 3465 hexahydrobromide, CAS 185991-07-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 51.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 141.00
50 mg	In stock	$ 243.00
100 mg	In stock	$ 383.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.03%

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Description	AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.
Targets&IC50	X4 HIV-1 (IIIB):12.3 nM (IC50, in MT-4 cells), HIV-2 (ROD):12.3 nM (IC50, in MT-4 cells), HIV-2 (EHO):12.3 nM (IC50, in MT-4 cells), X4 HIV-1 (NL4.3):6.1 nM (IC50, in MT-4 cells), X4 HIV-1 (HE):9.8 nM (IC50, in MT-4 cells), CXCL12 (AF647)-CXCR4:18 nM (IC50, in SupT1 cells), 12G5 mAb-CXCR4:0.75 nM (IC50, in SupT1 cells), X4 HIV-1 (NL4.3AMD3100):2822 nM (IC50, in MT-4 cells), X4 HIV-1 (RF):7.4 nM (IC50, in MT-4 cells)
In vitro	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].
In vivo	Administering 2.5 mg/kg/d of AMD 3465 subcutaneously for five weeks significantly inhibits the growth of U87 glioblastoma multiforme (GBM) and Daoy medulloblastoma xenografts.

Synonyms	GENZ-644494 (hexahydrobromide)
Molecular Weight	896.07
Formula	C24H44Br6N6
CAS No.	185991-07-5

Storage

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

Solubility Information

H2O: 38 mg/mL (42.41 mM)

DMSO: 50 mg/mL (55.80 mM), Sonification is recommended.

References and Literature

2. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Anti-Cancer Active Compound Library NO PAINS Compound Library Immunology/Inflammation Compound Library Immuno-Oncology Compound Library Anti-Cancer Compound Library Chemokine Inhibitor Library Cytokine Inhibitor Library Target-Focused Phenotypic Screening Library

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Keywords

AMD 3465 hexahydrobromide 185991-07-5 Autophagy GPCR/G Protein Immunology/Inflammation Microbiology/Virology Proteases/Proteasome CXCR HIV Protease Inhibitor AMD-3465 Hexahydrobromide GENZ 644494 AMD3465 GENZ-644494 (hexahydrobromide) HIV AMD 3465 Hexahydrobromide GENZ644494 CXC chemokine receptors GENZ-644494 hexahydrobromide inhibit AMD3465 Hexahydrobromide AMD-3465 AMD 3465 Human immunodeficiency virus GENZ-644494 inhibitor

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