AMD 3465 (Synonyms: GENZ-644494)

Name: AMD 3465
Brand: MedChemExpress
SKU: HY-15971A
Rating: 5.0 (5 reviews)

Cat. No.: HY-15971A Purity: 99.59%: FAQs
Data Sheet SDS COA Handling Instructions

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AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12^AF647 to CXCR4, with IC₅₀s of 0.75 nM and 18 nM in SupT1 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.

For research use only. We do not sell to patients.

AMD 3465 Chemical Structure

CAS No. : 185991-24-6

Size	Price	Stock	Quantity
5 mg	USD 186	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of AMD 3465:

AMD 3465 hexahydrobromide In-stock

4 Publications Citing Use of MCE AMD 3465

: AMD 3465 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2021 Mar 24;138:111476. [Abstract]; The results of western blotting showed that high glucose inhibited the activation of the cell cycle pathway, the expression level of CDK4, CDK6, Nusap1, and Cyclin D1 are reduced. However, under the action of AMD3465 (10 μM), the expression level of proteins is significantly higher than that of the HG group.

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HIV HIV-1 HIV-2

Biological Activity
Protocol
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

12G5 mAb-CXCR4

0.75 nM (IC₅₀, in SupT1 cells)

CXCL12^AF647-CXCR4

18 nM (IC₅₀, in SupT1 cells)

X4 HIV-1 (III_B)

12.3 nM (IC₅₀, in MT-4 cells)

X4 HIV-1 (NL4.3)

6.1 nM (IC₅₀, in MT-4 cells)

X4 HIV-1 (NL4.3^AMD3100)

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)

In Vitro

AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12^AF647 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

410.60

Formula

C₂₄H₃₈N₆

CAS No.

185991-24-6

Appearance

Solid-Liquid Mixture

Color

Off-white to light yellow

SMILES

C1(CNCC2=CC=C(CN3CCNCCCNCCNCCC3)C=C2)=NC=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

H₂O : ≥ 100 mg/mL (243.55 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4355 mL	12.1773 mL	24.3546 mL
5 mM	0.4871 mL	2.4355 mL	4.8709 mL
10 mM	0.2435 mL	1.2177 mL	2.4355 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.59%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (246 KB) HNMR (263 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61. [Content Brief]

[2]. Yang L, et al. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Res. 2007 Jan 15;67(2):651-8. [Content Brief]

Cell Assay ^[2]	Following serum starvation for 24 h, astrocytes, granule cells, U87 cells, and Daoy cells are treated with 1 μg/mL CXCL12, 2.5 ng/mL AMD 3465, 200 μM rolipram, or 10 μM forskolin. Daoy and U87 cell growth in culture is measured by trypan blue exclusion after 24 and 48 h of treatment, respectively^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] Mice are imaged at least twice after implantation of cells to identify those with equivalent tumor growth rates. Two weeks after tumor cell implantation, cohorts of mice with approximately equivalent tumor bioluminescence are divided into equal control and treatment groups. Animals in AMD 3465 experiments receive s.c. osmotic pumps loaded with 10 mg/mL AMD 3465 in sterile PBS or PBS alone. The infusion rate is 0.25 μL/h (50 μg/d). For the experiments with rolipram or caffeine, mice in the treatment groups receive oral administration of rolipram (5 μg/g/d) or caffeine (100 μg/g/d). The concentration of drug in the water is determined from daily measurements of water consumption by each animal over the course of 7 days. Concentrations are adjusted based on water consumption to provide the prescribed dose^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61. [Content Brief] [2]. Yang L, et al. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Res. 2007 Jan 15;67(2):651-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	2.4355 mL	12.1773 mL	24.3546 mL	60.8865 mL
	5 mM	0.4871 mL	2.4355 mL	4.8709 mL	12.1773 mL
	10 mM	0.2435 mL	1.2177 mL	2.4355 mL	6.0887 mL
	15 mM	0.1624 mL	0.8118 mL	1.6236 mL	4.0591 mL
	20 mM	0.1218 mL	0.6089 mL	1.2177 mL	3.0443 mL
	25 mM	0.0974 mL	0.4871 mL	0.9742 mL	2.4355 mL
	30 mM	0.0812 mL	0.4059 mL	0.8118 mL	2.0296 mL
	40 mM	0.0609 mL	0.3044 mL	0.6089 mL	1.5222 mL
	50 mM	0.0487 mL	0.2435 mL	0.4871 mL	1.2177 mL
	60 mM	0.0406 mL	0.2030 mL	0.4059 mL	1.0148 mL
	80 mM	0.0304 mL	0.1522 mL	0.3044 mL	0.7611 mL
	100 mM	0.0244 mL	0.1218 mL	0.2435 mL	0.6089 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

AMD 3465 Related Classifications

Infection Endocrinology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMD 3465185991-24-6GENZ-644494AMD3465AMD-3465GENZ644494GENZ 644494CXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusInhibitorinhibitorinhibit

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AMD 3465 (Synonyms: GENZ-644494)

Customer Review

Other Forms of AMD 3465:

AMD 3465 Related Antibodies

4 Publications Citing Use of MCE AMD 3465

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CXCR Isoform Specific Products:

View All HIV Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

AMD 3465 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

AMD 3465 Related Classifications

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