1. Epigenetics
    PI3K/Akt/mTOR
  2. AMPK
  3. ASP4132

ASP4132 

Cat. No.: HY-136447 Purity: 98.85%
Handling Instructions

ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.

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

ASP4132 Chemical Structure

ASP4132 Chemical Structure

CAS No. : 1640294-30-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 258 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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Description

ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models[1].

IC50 & Target[1]

AMPK

18 nM (EC50)

In Vitro

ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell[1].
ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM)[1].

In Vivo

ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression[1].
ASP4132 (1 mg/kg; IV or PO) has a T1/2 of 3.6 hours, a CLtot of 19 mL/min•kg, and a Vss of 4.6 L/kg for rats for IV[1].
ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min•kg)[1].

Animal Model: Five-week-old male nude mice with MDA-MB-453[1]
Dosage: 0.5, 1, 2, 4, 8 mg/kg
Administration: PO; once daily; for 21 days
Result: The tumor growth inhibition (TGI) rate was 29% at 1 mg/kg, and the tumor regression rate was 26%, 87% and 96% at 2, 4 and 8 mg/kg, respectively.
Animal Model: Male SD rats[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had a T1/2 of 3.6 hours, a CLtot of 19 mL/min•kg, and a Vss of 4.6 L/kg for rats for IV.
Had a Cmax of 72 ng/mL and an AUC24h of 705 ng∙h/mL for PO.
Molecular Weight

937.06

Formula

C₄₆H₅₁F₃N₆O₈S₂

CAS No.

1640294-30-9

SMILES

O=C(C1=NC2=CC=C(C3CCN(CC4=CC=C(OC)N=C4)CC3)C=C2N1)N5CCN(CC6=CC=C(C(F)(F)F)C=C6)CC5.O=S(C7=CC=C(C)C=C7)(O)=O.O=S(C8=CC=C(C)C=C8)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (266.79 mM; Need ultrasonic)

Methanol : 8.33 mg/mL (8.89 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0672 mL 5.3358 mL 10.6717 mL
5 mM 0.2134 mL 1.0672 mL 2.1343 mL
10 mM 0.1067 mL 0.5336 mL 1.0672 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6.25 mg/mL (6.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6.25 mg/mL (6.67 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (6.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ASP4132ASP 4132ASP-4132AMPKAMP-activated protein kinaseorallyanti-cancerbreastcancerxenograftMDA-MB-453Inhibitorinhibitorinhibit

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