AMD 3465 hexahydrobromide

SKU: orb1218571

Description

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

Key Properties

• CAS Number: 185991-07-5
• MW: 896.07
• Purity: >98% (HPLC)
• Formula: C₂₄H₄₄Br₆N₆
• SMILES: C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CNCC3=CC=CC=N3.Br.Br.Br.Br.Br.Br
• Target: CXCR
• Solubility: DMSO:50 mg/mL (55.80 mM; Need ultrasonic);H2O: 38 mg/mL (42.41 mM)

Bioactivity

• In Vivo:
  AMD 3465 (2.5 mg/kg/d, s. c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts.
• In Vitro:
  AMD 3465 hexahydrobromide 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. 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GENZ-644494 (hexahydrobromide)

Quick Database Links

Gene Symbol

CXCR