ASP4132 |
カタログ番号GC60058
One-Click Copy Product Info
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ASP4132 は、18 nM の EC50 を持つ、経口で活性な強力な AMPK アクティベーターです。 ASP4132 には抗がん作用があり、乳がん異種移植マウスモデルで腫瘍を退縮させます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1640294-30-9
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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]
[1]. Kazuyuki Kuramoto, et al. Development of a Potent and Orally Active Activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK), ASP4132, as a Clinical Candidate for the Treatment of Human Cancer. Bioorg Med Chem. 2020 Mar 1;28(5):115307.
| Cas No. | 1640294-30-9 | SDF | |
| Canonical 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 | ||
| Formula | C46H51F3N6O8S2 | M.Wt | 937.06 |
| 溶解度 | DMSO: 250 mg/mL (266.79 mM); Methanol: 8.33 mg/mL (8.89 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.0672 mL | 5.3358 mL | 10.6717 mL |
| 5 mM | 213.4 μL | 1.0672 mL | 2.1343 mL |
| 10 mM | 106.7 μL | 533.6 μL | 1.0672 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)