AMD 3465 hexahydrobromide (Synonyms: GENZ-644494 hexahydrobromide)

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

Cat. No.: HY-15971 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) 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 hexahydrobromide Chemical Structure

CAS No. : 185991-07-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 87	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 87	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 61	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 286	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 528	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 hexahydrobromide:

AMD 3465 Get quote

4 Publications Citing Use of MCE AMD 3465 hexahydrobromide

: AMD 3465 hexahydrobromide 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
Customer Review

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 (NL4.3)

6.1 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)

X4 HIV-1 (III_B)

12.3 nM (IC₅₀, in MT-4 cells)

X4 HIV-1 (NL4.3^AMD3100)

2822 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 hexahydrobromide 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

896.07

Formula

C₂₄H₄₄Br₆N₆

CAS No.

185991-07-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Br.[H]Br.[H]Br.[H]Br.[H]Br.[H]Br.C1(CNCC2=CC=C(CN3CCNCCCNCCNCCC3)C=C2)=NC=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (55.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 38 mg/mL (42.41 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1160 mL	5.5799 mL	11.1598 mL
5 mM	0.2232 mL	1.1160 mL	2.2320 mL
10 mM	0.1116 mL	0.5580 mL	1.1160 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 (sealed storage, away from moisture). 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (111.60 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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: ≥98.0%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (250 KB) HNMR (206 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 / DMSO	1 mM	1.1160 mL	5.5799 mL	11.1598 mL	27.8996 mL
	5 mM	0.2232 mL	1.1160 mL	2.2320 mL	5.5799 mL
	10 mM	0.1116 mL	0.5580 mL	1.1160 mL	2.7900 mL
	15 mM	0.0744 mL	0.3720 mL	0.7440 mL	1.8600 mL
	20 mM	0.0558 mL	0.2790 mL	0.5580 mL	1.3950 mL
	25 mM	0.0446 mL	0.2232 mL	0.4464 mL	1.1160 mL
	30 mM	0.0372 mL	0.1860 mL	0.3720 mL	0.9300 mL
	40 mM	0.0279 mL	0.1395 mL	0.2790 mL	0.6975 mL
DMSO	50 mM	0.0223 mL	0.1116 mL	0.2232 mL	0.5580 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 hexahydrobromide 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 3465 hexahydrobromide185991-07-5GENZ-644494 hexahydrobromideCXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusInhibitorinhibitorinhibit

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AMD 3465 hexahydrobromide (Synonyms: GENZ-644494 hexahydrobromide)

Customer Review

Other Forms of AMD 3465 hexahydrobromide:

AMD 3465 hexahydrobromide Related Antibodies

4 Publications Citing Use of MCE AMD 3465 hexahydrobromide

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•Related Screening Libraries:

•Related Small Molecules:

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View All CXCR Isoform Specific Products:

View All HIV Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

AMD 3465 hexahydrobromide Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

AMD 3465 hexahydrobromide Related Classifications

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