| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| 10mg | |||
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| Targets |
AMA-37 targets DNA-dependent protein kinase (DNA-PK), a serine/threonine protein kinase that plays a critical role in the non-homologous end joining (NHEJ) pathway of DNA double-strand break repair. DNA-PK is activated upon binding to DNA ends and is essential for repairing DNA damage. AMA-37 is a selective, reversible, and ATP-competitive inhibitor of DNA-PK, with an IC50 of 0.27 μM. It also inhibits other kinases, including p110α, p110β, and p110γ, but with lower potency. By inhibiting DNA-PK, AMA-37 impairs DNA repair, making cancer cells more sensitive to DNA-damaging agents such as radiation and chemotherapeutic drugs.
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| ln Vitro |
Inhibiting PI3K is less successful with AMA-37 [2]. The ability of UCN-01, isogranimide, and debromohymenaldolase to bypass G2 block (ρ < 0.05) is reduced by AMA-37 (20 μM), but not by caffeine [3]. Radiosensitization is the outcome of using AMA37 to inhibit DNA-PK [3].
In vitro, AMA-37 is a potent inhibitor of DNA-PK, with an IC50 of 0.27 μM. It also inhibits p110α (IC50 = 32 μM), p110β (IC50 = 3.7 μM), and p110γ (IC50 = 22 μM). Its activity is typically measured using kinase assays with recombinant DNA-PK and a peptide substrate. In cell-based assays, AMA-37 has been shown to inhibit DNA-PK activity and to sensitize cancer cells to ionizing radiation and chemotherapeutic agents that induce DNA double-strand breaks. |
| ln Vivo |
In vivo, AMA-37 is used to study the role of DNA-PK in DNA repair and to explore potential strategies for radiosensitization in cancer therapy. By inhibiting DNA-PK, it can enhance the effectiveness of radiation therapy. However, specific in vivo protocols and results, such as efficacy in animal models, are not detailed in the available literature. Its use is limited to research applications to validate DNA-PK as a therapeutic target for cancer.
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| Enzyme Assay |
The in vitro assays for AMA-37 measure its inhibition of DNA-PK kinase activity. Kinase assays are performed using recombinant DNA-PK, a peptide substrate, and ATP in the presence of varying concentrations of AMA-37. The incorporation of phosphate into the substrate is measured, and the IC50 is determined from the dose-response curve. To assess selectivity, the compound is tested against a panel of other kinases, including p110α, p110β, and p110γ.
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| Cell Assay |
In vitro cell-based assays for AMA-37 are used to study its effects on DNA repair and radiosensitivity. Cancer cells are treated with AMA-37, and the accumulation of DNA damage is assessed by measuring the levels of phosphorylated H2AX (γ-H2AX) foci, a marker of DNA double-strand breaks. Cell viability is assessed after radiation exposure to determine the compound's ability to enhance radiosensitivity. These cell-based assays confirm that AMA-37 inhibits DNA-PK, disrupts DNA repair, and enhances cellular radiosensitivity.
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| Animal Protocol |
In vivo animal experiments for AMA-37 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a DNA-PK inhibitor like AMA-37 would involve its administration to tumor-bearing mice in combination with radiation therapy. The compound would be formulated for injection, and tumor growth and response to radiation would be assessed. However, specific protocols for AMA-37 are not detailed.
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| ADME/Pharmacokinetics |
AMA-37 has a molecular formula of C17H17NO3. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage as a dry powder.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for AMA-37 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. AMA-37 is an inhibitor of DNA-PK, and its toxicity would be related to its effects on DNA repair in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling AMA-37. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References |
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| Additional Infomation |
[2-Hydroxy-4-(4-morpholino)phenyl]-phenyl ketone is a benzophenone compound.
AMA-37 (DNA-PK Inhibitor V) is a research compound and is not approved for any clinical or therapeutic use. It is a synthetic arylmorpholine small molecule that functions as a selective, reversible, and ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK). It has an IC50 of 0.27 μM for DNA-PK. AMA-37 also inhibits other kinases, including p110α, p110β, and p110γ. It is used in research to study the role of DNA-PK in DNA repair, particularly in the context of cancer and radiosensitization. Its mechanism of action involves inhibiting DNA-PK, thereby impairing DNA repair and sensitizing cancer cells to DNA-damaging agents. |
| Molecular Formula |
C17H17NO3
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|---|---|
| Molecular Weight |
283.32
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| Exact Mass |
283.121
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| CAS # |
404009-46-7
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| PubChem CID |
16760391
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| Appearance |
White to yellow solid powder
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| LogP |
2.524
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
348
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FALILNHGILFDLC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17NO3/c19-16-12-14(18-8-10-21-11-9-18)6-7-15(16)17(20)13-4-2-1-3-5-13/h1-7,12,19H,8-11H2
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| Chemical Name |
(2-hydroxy-4-morpholin-4-ylphenyl)-phenylmethanone
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| Synonyms |
AMA-37 AMA37 AMA 37
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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 |
| 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 (~352.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.82 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 (8.82 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5296 mL | 17.6479 mL | 35.2958 mL | |
| 5 mM | 0.7059 mL | 3.5296 mL | 7.0592 mL | |
| 10 mM | 0.3530 mL | 1.7648 mL | 3.5296 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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