AMXT-1501 tetrahydrochloride

Name: AMXT-1501 tetrahydrochloride
Brand: MedChemExpress
SKU: HY-124617A
Rating: 5.0 (5 reviews)

Cat. No.: HY-124617A Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines.

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

AMXT-1501 tetrahydrochloride Chemical Structure

CAS No. : 2444815-84-1

Size	Price	Stock	Quantity
1 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1850	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2850	In-stock	Estimated Time of Arrival: December 31
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200 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of AMXT-1501 tetrahydrochloride:

AMXT-1501 Get quote

5 Publications Citing Use of MCE AMXT-1501 tetrahydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells^[1]. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines^[2].

IC₅₀ & Target

Polyamine transport^[1]

In Vitro

AMXT-1501 tetrahydrochloride (0.39-50 µM; 48 hours) treatment exhibits cytotoxicity against this panel of NB cell lines (BE(2)-C, SMS-KCNR and SH-SY5Y cells), with IC₅₀ values of 17.72 µM for SMS-KCNR, 17.69 µM for BE(2)-C, and 14.13 µM for SH-SY5Y^[2].
BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells are exposed to AMXT-1501 tetrahydrochloride (2.5 µM) and DFMO (2.5 mM) alone or in combination (AMXT-1501 tetrahydrochloride 2.5 µM + DFMO 2.5 mM). After 96 hours exposure to AMXT-1501 tetrahydrochloride or DFMO does not significantly alter the level of noncleaved PARP, cleaved PARP and cleaved caspase 3, whereas cells treated with the combination of AMXT-1501 tetrahydrochloride with DFMO decrease the amount of noncleaved PARP and increase the amount of cleaved PARP and cleaved caspase 3^[2].

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

Cell Viability Assay^[2]

Cell Line:	BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells
Concentration:	0.39 µM, 1 µM, 3.1 µM, 10 µM, 31 µM, 50 µM
Incubation Time:	48 hours
Result:	AMXT-1501 tetrahydrochloride exhibited cytotoxicity against this panel of NB cell lines.

Western Blot Analysis^[2]

Cell Line:	BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells
Concentration:	2.5 µM
Incubation Time:	72 hours
Result:	Combination treatment with DFMO decreased the amount of noncleaved PARP and increased the amount of cleaved PARP and cleaved caspase 3 in all three cell lines.

In Vivo

AMXT-1501 tetrahydrochloride (3 mg/kg; subcutaneous injection; every day; 28 days) alone is sufficient to delay EAE onset moderately,but fails to protect animals from reaching the endpoint. However, the combination of DFMO and AMXT-1501 tetrahydrochloride are sufficient to deplete T cell polyamine pool, and consequently suppress T cell proliferation and effector function in vivo^[3].

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

Animal Model:	C57BL/6 (WT) and ODC knockout strain (ODC cKO) mice bearing experimental autoimmune encephalomyelitis (EAE) model ^[3]
Dosage:	3 mg/kg
Administration:	Subcutaneous injection; every day; 28 days
Result:	Displayed a delayed disease onset initially, but eventually proceeded with pathologic development and reached the endpoint.

Clinical Trial

Molecular Weight

714.77

Formula

C₃₂H₇₂Cl₄N₆O₂

CAS No.

2444815-84-1

Appearance

Solid

Color

White to off-white

SMILES

CCCCCCCCCCCCCCCC(NCCCC[C@@H](N)C(NCCCNCCCCNCCCN)=O)=O.Cl.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility

In Vitro:

H₂O : 83.33 mg/mL (116.58 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3991 mL	6.9953 mL	13.9905 mL
5 mM	0.2798 mL	1.3991 mL	2.7981 mL
10 mM	0.1399 mL	0.6995 mL	1.3991 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 and 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.

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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:

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: 50 mg/mL (69.95 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 (272 KB) SDS (251 KB)

COA (240 KB) HNMR (295 KB)

Handling Instructions (2659 KB)

References

[1]. Candace S Hayes, et al. Polyamine-blocking therapy reverses immunosuppression in the tumor microenvironment. Cancer Immunol Res. 2014 Mar;2(3):274-85. [Content Brief]

[2]. Katherine Samal, et al. AMXT‐1501, a novel polyamine transport inhibitor, synergizes with DFMO in inhibiting neuroblastoma cell proliferation by targeting both ornithine decarboxylase and polyamine transport. Int J Cancer. 2013 Sep 15;133(6):1323-33. [Content Brief]

[3]. Ruohan Wu, et al. De novo synthesis and salvage pathway coordinately regulate polyamine homeostasis and determine T cell proliferation and function. Sci Adv. 2020 Dec 16;6(51):eabc4275. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O	1 mM	1.3991 mL	6.9953 mL	13.9905 mL	34.9763 mL
	5 mM	0.2798 mL	1.3991 mL	2.7981 mL	6.9953 mL
	10 mM	0.1399 mL	0.6995 mL	1.3991 mL	3.4976 mL
	15 mM	0.0933 mL	0.4664 mL	0.9327 mL	2.3318 mL
	20 mM	0.0700 mL	0.3498 mL	0.6995 mL	1.7488 mL
	25 mM	0.0560 mL	0.2798 mL	0.5596 mL	1.3991 mL
	30 mM	0.0466 mL	0.2332 mL	0.4664 mL	1.1659 mL
	40 mM	0.0350 mL	0.1749 mL	0.3498 mL	0.8744 mL
	50 mM	0.0280 mL	0.1399 mL	0.2798 mL	0.6995 mL
	60 mM	0.0233 mL	0.1166 mL	0.2332 mL	0.5829 mL
	80 mM	0.0175 mL	0.0874 mL	0.1749 mL	0.4372 mL
	100 mM	0.0140 mL	0.0700 mL	0.1399 mL	0.3498 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.