1. Apoptosis
  2. Apoptosis
  3. AMXT-1501 tetrahydrochloride

AMXT-1501 tetrahydrochloride 

Cat. No.: HY-124617A Purity: ≥98.0%
Handling Instructions

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

AMXT-1501 tetrahydrochloride Chemical Structure

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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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Based on 1 publication(s) in Google Scholar

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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].

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].

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

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: ≥98.0%

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Keywords:

AMXT-1501 tetrahydrochlorideApoptosispolyaminetumorInhibitorinhibitorinhibit

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AMXT-1501 tetrahydrochloride
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