化合物AMD 3465 hexahydrobromide T7208

Product Introduction
Bioactivity


英文名: AMD 3465 hexahydrobromide

描述: AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) 是一种 CXCR4受体拮抗剂，具有潜在的抗癌和抗 HIV 活性。

体外活性: 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].

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

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

溶解度: H2O : 38 mg/mL (42.41 mM)
DMSO : 50 mg/mL (55.80 mM)


关键字: Inhibitor | AMD 3465 hexahydrobromide | AMD-3465 Hexahydrobromide | GENZ 644494 | AMD3465 | CXCR | HIV | AMD 3465 Hexahydrobromide | GENZ644494 | CXC chemokine receptors | GENZ-644494 hexahydrobromide | inhibit | AMD3465 Hexahydrobromide | AMD-3465 | AMD 3465 | Human immunodeficiency virus | GENZ-644494

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相关库: Membrane Protein-targeted Compound Library | Macrocyclic Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Chemokine Inhibitor Library | Autophagy Compound Library | Anti-Viral Compound Library | Anti-Infection Compound Library

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