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Purity: ≥98%
ASP4132 tosylate (ASP-4132) is an oral bioavailable AMPK activator (EC50 = 18 nM) with potential anticancer activity. Upon oral administration, ASP4132 affects oxidative phosphorylation in mitochondria of metabolically-active tumor cells, which reduces both energy production and tumor cell proliferation. Mitochondrial oxidative phosphorylation is hyperactivated in tumor cells and plays a key role in the promotion of tumor cell proliferation.
| ln Vitro |
Comparable cell growth inhibitory action (IC50=0.014 μM) is demonstrated by ASP4132 against MDA-MB-453 breast cancer cells[1]. Against SK-BR-3, ASP4132 exhibits very poor antiproliferative action (IC50>3 μM)[1].
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| ln Vivo |
ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor development 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].
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| Animal Protocol |
Animal/Disease Models: Fiveweeks old male nude mice with MDA-MB-453[1]
Doses: 0.5, 1, 2, 4, 8 mg/kg Route of Administration: PO; one time/day; for 21 days Experimental Results: 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/Disease Models: Male SD rats[1] Doses: 1 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: IV or PO Experimental Results: Had a T1/2 of 3.6 hrs (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. |
| References | |
| Additional Infomation |
ASP4132 is a molecule with potential antineoplastic activity. Upon oral administration, ASP4132 affects oxidative phosphorylation in mitochondria of metabolically-active tumor cells, which reduces both energy production and tumor cell proliferation. Mitochondrial oxidative phosphorylation is hyperactivated in tumor cells and plays a key role in the promotion of tumor cell proliferation.
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| Molecular Formula |
C46H51F3N6O8S2
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|---|---|
| Molecular Weight |
937.0578
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| Exact Mass |
936.316
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| Elemental Analysis |
C, 58.96; H, 5.49; F, 6.08; N, 8.97; O, 13.66; S, 6.84
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| CAS # |
1640294-30-9
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| Related CAS # |
1640294-29-6;1640294-30-9;
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| PubChem CID |
146673134
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
65
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KDMGCEXVMOJAAC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H35F3N6O2.2C7H8O3S/c1-43-29-9-4-23(19-36-29)21-39-12-10-24(11-13-39)25-5-8-27-28(18-25)38-30(37-27)31(42)41-16-14-40(15-17-41)20-22-2-6-26(7-3-22)32(33,34)352*1-6-2-4-7(5-3-6)11(8,9)10/h2-9,18-19,24H,10-17,20-21H2,1H3,(H,37,38)2*2-5H,1H3,(H,8,9,10)
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| Chemical Name |
(6-(1-((6-methoxypyridin-3-yl)methyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-yl)(4-(4-(trifluoromethyl)benzyl)piperazin-1-yl)methanone bis(4-methylbenzenesulfonate)
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| Synonyms |
ASP-4132ASP4132 tosylate ASP 4132 ASP4132
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~106.72 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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