AMD 3465 hexahydrobromide
作者：齊岳
發(fā)布時(shí)間：2023-09-12
09:09:44
點(diǎn)擊數(shù)：
產(chǎn)品名稱：AMD 3465 hexahydrobromide
產(chǎn)品描述：
| 產(chǎn)品描述 | AMD 3465 hexahydrobromide is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity. |
| 靶點(diǎn)活性 | X4 HIV-1 (NL4.3AMD3100):2822 nM (IC50, in MT-4 cells), X4 HIV-1 (IIIB):12.3 nM (IC50, in MT-4 cells), X4 HIV-1 (RF):7.4 nM (IC50, in MT-4 cells), 12G5 mAb-CXCR4:0.75 nM (IC50, in SupT1 cells), HIV-2 (ROD):12.3 nM (IC50, in MT-4 cells), CXCL12AF647-CXCR4:18 nM (IC50, in SupT1 cells), X4 HIV-1 (HE):9.8 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) |
| 體外活性 | 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]. |
| 體內(nèi)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] |
| 別名 | GENZ-644494 (hexahydrobromide) |
| 分子量 | 896.07 |
| 分子式 | C24H44Br6N6 |
| CAS No. | 185991-07-5 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 38 mg/mL (42.41 mM)
DMSO: 50 mg/mL (55.80 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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