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AMD 3465
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AMD 3465图片
CAS NO:185991-24-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
GENZ-644494
产品介绍
AMD 3465 (GENZ-644494) 是一种有效的CXCR4拮抗剂,在 SupT1 细胞中,能够抑制 12G5 mAb,CXCL12AF647CXCR4结合,IC50值分别为 0.75 nM 和 18 nM;AMD 3465 同时可有效抑制X4 HIV的复制 (IC50,1-10 nM),但对 R5 HIV 病毒无作用。
生物活性

AMD 3465 (GENZ-644494) is a potent antagonist ofCXCR4, inhibits binding of 12G5 mAb and CXCL12AF647toCXCR4, withIC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication ofX4HIVstrains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

IC50& Target[1]

12G5 mAb-CXCR4

0.75 nM (IC50, in SupT1 cells)

CXCL12AF647-CXCR4

18 nM (IC50, in SupT1 cells)

X4 HIV-1 (IIIB)

12.3 nM (IC50, in MT-4 cells)

X4 HIV-1 (NL4.3)

6.1 nM (IC50, in MT-4 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)

X4 HIV-1 (HE)

9.8 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)

体外研究
(In Vitro)

AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647to 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 IC50of 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 IC50ranging from 6 to 12 nM. The IC50for 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].

体内研究
(In Vivo)

AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts[2].

分子量

410.60

Formula

C24H38N6

CAS 号

185991-24-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.