PeptideDB

AMA-37 404009-46-7

AMA-37 404009-46-7

CAS No.: 404009-46-7

AMA-37 is an analog of Arylmorpholine and an ATP-competitive DNA-PK inhibitor. Its IC50s are 0.27 μM (DNA-PK), 32 μM (
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

AMA-37 is an analog of Arylmorpholine and an ATP-competitive DNA-PK inhibitor. Its IC50s are 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ). ).

Physicochemical Properties


Molecular Formula C17H17NO3
Molecular Weight 283.32
Exact Mass 283.121
CAS # 404009-46-7
PubChem CID 16760391
Appearance White to yellow solid powder
LogP 2.524
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 3
Heavy Atom Count 21
Complexity 348
Defined Atom Stereocenter Count 0
InChi Key FALILNHGILFDLC-UHFFFAOYSA-N
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
Chemical Name

(2-hydroxy-4-morpholin-4-ylphenyl)-phenylmethanone
Synonyms

AMA-37 AMA37 AMA 37
HS Tariff Code 2934.99.9001
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)

Biological Activity


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].
References

[1]. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

[2]. Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold. Bioorg Med Chem. 2004 Sep 1;12(17):4749-59.

[3]. Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage. Mol Cancer Ther. 2006 Apr;5(4):885-92.

Additional Infomation [2-hydroxy-4-(4-morpholinyl)phenyl]-phenylmethanone is a member of benzophenones.

Solubility Data


Solubility (In Vitro) DMSO : ~100 mg/mL (~352.96 mM)
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.