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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $34 | In Stock | |
5 mg | $51 | In Stock | |
10 mg | $72 | In Stock | |
25 mg | $141 | In Stock | |
50 mg | $243 | In Stock | |
100 mg | $383 | In Stock | |
1 mL x 10 mM (in DMSO) | $61 | In Stock |
Description | AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity. |
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. |
Alias | 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) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/H2O
DMSO
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