AZ20 [1233339-22-4]
Katalog-Nummer HY-15557-1ml
Size : 10mM/1mL
Marke : MedChemExpress
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AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
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AZ20 Chemische Struktur
CAS. Nr. : 1233339-22-4
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- Tumor pieces from M130116 PDXs treated with the vehicle or the RVX2135/AZ20 combination treatment are subjected to western blot analysis.
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| AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM). | |||
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| In Vitro | AZ20 inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC50 of 5 nM and ATR mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma tumor cells with an IC50 of 50 nM. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | ||
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| Compound dose ranges are created by diluting in 100% DMSO and then further into assay medium (EMEM, 10% FCS, 1% glutamine) using a Labcyte Echo acoustic dispensing instrument. Cells are plated in 384-well Costar plates at 9×104 cells per mL in 40 μL of EMEM, 10% FCS, 1% glutamine and grown for 24 h. Following addition of compound the cells are incubated for 60 min. A final concentration of 3 μM 4NQO (prepared in 100% DMSO) is then added using the Labcyte Echo, and the cells are incubated for a further 60 min. The cells are fixed by adding 40 μL of 3.7% v/v formaldehyde solution for 20 min. After removal of fix, cells are washed with PBS and permeabilized in 40 μL of PBS containing 0.1% Triton X-100. The cells are then washed, and 15 μL primary antibody solution (pChk1 Ser345) is added. The plates are incubated at 4°C overnight. The primary antibody is then washed off, and 20 μL of secondary antibody solution and 1 μM Hoechst 33258 added for 90 min at room temperature. The plates are washed and left in 40 μL of PBS. Plates are then read on an ArrayScan VTI instrument to determine staining intensities, and dose responses are obtained and used to determine the IC50 values for the compounds. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz. |
| Female Swiss nu/nu mice are housed in negative pressure isolators. LoVo tumor xenografts are established in 8- to 12-week-old mice by injecting 1×107 tumor cells subcutaneously (100 μL in serum free medium) on the left dorsal flank. Animals are randomized into treatment groups when tumors become palpable. AZ20 is prepared in 10% DMSO/40% propylene glycol/50% water and administered orally. Tumors are measured up to three times per week with calipers. Tumor volumes are calculated and the data plotted using the geometric mean for each group versus time. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz. |
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[1]. Foote KM, et al. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. J Med Chem. 2013 Mar 14
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|
| DMSO | 1 mM | 2.4242 mL | 12.1209 mL | 24.2418 mL | 60.6046 mL |
| 5 mM | 0.4848 mL | 2.4242 mL | 4.8484 mL | 12.1209 mL | |
| 10 mM | 0.2424 mL | 1.2121 mL | 2.4242 mL | 6.0605 mL | |
| 15 mM | 0.1616 mL | 0.8081 mL | 1.6161 mL | 4.0403 mL | |
| 20 mM | 0.1212 mL | 0.6060 mL | 1.2121 mL | 3.0302 mL | |
| 25 mM | 0.0970 mL | 0.4848 mL | 0.9697 mL | 2.4242 mL | |
| 30 mM | 0.0808 mL | 0.4040 mL | 0.8081 mL | 2.0202 mL | |
| 40 mM | 0.0606 mL | 0.3030 mL | 0.6060 mL | 1.5151 mL | |
| 50 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2121 mL | |
| 60 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0101 mL | |
| 80 mM | 0.0303 mL | 0.1515 mL | 0.3030 mL | 0.7576 mL | |
| 100 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6060 mL |
- Cell Cycle/DNA Damage PI3K/Akt/mTOR
- ATM/ATR
- Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
AZ201233339-22-4AZ 20AZ-20ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit
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