AMD 3465 hexahydrobromide is a potent, selective CXCR4 antagonist and exhibits 8-fold higher affinity than AMD 3100 and inhibits SDF-1α-ligand binding (Ki = 41.7 nM).
AMD 3465 6HBr 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bone-Un cells
100 nM
30 minutes
AMD3465 reduced the LASP1-Ago2 interaction
Cancers (Basel). 2020 Aug 29;12(9):2455.
Human PBMCs
1.3 nM
inhibition of SHIV-89.6P replication
Proc Natl Acad Sci U S A. 2008;105(30):10531-10536.
Human PBMCs
2.2 nM
inhibition of SHIV-KU1 replication
Proc Natl Acad Sci U S A. 2008;105(30):10531-10536.
SuDHL8
500 μM
5 min
Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed AMD3465 partially inhibited the binding of [18F]MCFB
Mol Pharm. 2019 May 6;16(5):2106-2117.
U2932
500 μM
5 min
Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed AMD3465 partially inhibited the binding of [18F]MCFB
Mol Pharm. 2019 May 6;16(5):2106-2117.
231S cells
100 nM
30 minutes
AMD3465 inhibited the CXCR4-dependent LASP1-Ago2 interaction
Cancers (Basel). 2020 Aug 29;12(9):2455.
AMD 3465 6HBr 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
Pancreatic cancer xenograft model
Intraperitoneal injection
10 mg/kg
Daily for 28 days
To evaluate the effect of AMD3465 in combination with temsirolimus to overcome temsirolimus resistance. Results showed that the combination therapy significantly inhibited tumor growth and reduced cyclin D1 and c-Myc gene expression.
Neoplasia. 2012 Aug;14(8):690-701.
CBA/J mice
Models of Th1- and Th2-cell-mediated pulmonary granuloma formation
Osmotic pump implantation
5 μg/hour (6 mg/kg/day)
Continuous delivery for 5 days
AMD3465 significantly abrogated type-2 inflammation with reductions in lesion size and eosinophil content as well as abrogated IL-5, IL-10, and IL-13 cytokine production in draining lymph nodes.
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