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Chemical Structure| 185991-07-5 Chemical Structure| 185991-07-5

Structure of AMD 3465 6HBr
CAS No.: 185991-07-5

Chemical Structure| 185991-07-5

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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).

Synonyms: GENZ-644494 hexahydrobromide; AMD 3465 hexahydrobromide; AMD 3465 (hydrobromide)

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Product Details of AMD 3465 6HBr

CAS No. :185991-07-5
Formula : C24H44Br6N6
M.W : 896.07
SMILES Code : [H]Br.[H]Br.[H]Br.[H]Br.[H]Br.[H]Br.C1(CNCC2=CC=C(CN3CCNCCCNCCNCCC3)C=C2)=NC=CC=C1
Synonyms :
GENZ-644494 hexahydrobromide; AMD 3465 hexahydrobromide; AMD 3465 (hydrobromide)
MDL No. :MFCD20926342

Safety of AMD 3465 6HBr

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of AMD 3465 6HBr

GPCR

Isoform Comparison

Biological Activity

Target
  • CXCR4

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone-Un cells 100 nM 30 minutes AMD3465 reduced the LASP1-Ago2 interaction PMC7564666
231S cells 100 nM 30 minutes AMD3465 inhibited the CXCR4-dependent LASP1-Ago2 interaction PMC7564666
MDA-MB-231 shCXCR4 0.5 μg/mL 24 h Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed CXCR4 knockdown reduced the uptake of [18F]MCFB PMC6522096
SuDHL8 500 μM 5 min Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed AMD3465 partially inhibited the binding of [18F]MCFB PMC6522096
U2932 500 μM 5 min Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed AMD3465 partially inhibited the binding of [18F]MCFB PMC6522096
Human osteosarcoma cells (U2OS) 300 nM 30 minutes Evaluate inhibition of cell migration, P-SS-AMD/miR-200c inhibited migration by 77% PMC5417087
HS766T cells 100 ng/ml 60 minutes To investigate the regulation of the mTOR pathway by SDF-1 α via CXCR4 activation. Results showed that SDF-1 α stimulation led to phosphorylation of Akt and S6-RP, indicating that CXCR4 activation can maintain mTOR pathway activity. PMC3432475

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice U2932 and SuDHL8 tumor models Intravenous injection 50 mg/kg Single dose, lasted for 30 min Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed metformin treatment significantly reduced the urinary excretion of [18F]MCFB PMC6522096
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. PMC3432475
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. PMC1599788

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.12mL

0.22mL

0.11mL

5.58mL

1.12mL

0.56mL

11.16mL

2.23mL

1.12mL

References

 

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