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CP-466722

Catalog No. T6261 CAS 1080622-86-1

Synonyms: CP 466722, CP466722

CP-466722, an effective and reversible ATM inhibitor, does not inhibit ATR and PI3K or PIKK family members in cells.

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CP-466722, CAS 1080622-86-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 193.00
50 mg	In stock	$ 312.00
100 mg	In stock	$ 506.00
500 mg	In stock	$ 1,130.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.85%

Purity: 99.14%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CP-466722, an effective and reversible ATM inhibitor, does not inhibit ATR and PI3K or PIKK family members in cells.
Targets&IC50	ATM:410 nM
In vitro	CP-466722 is used as a potential inhibitor to inhibits the activity of ATM kinase, which phosphorylates GST-p53(1–101) substrate. CP-466722 also exhibits the decreasing activities against abl and src kinases. In MCF-7 human breast cancer cells and primary and immortalized diploid human fibroblasts, CP-466722 suppress ATM-dependent p53 induction. In HeLa cells, CP-466722(6 μM), leads to the inhibition in ATM-dependent phosphorylation by reversibly inhibiting ionizing radiation (IR)-induced ATM kinase activity.
Kinase Assay	In vitro kinase assays [1] : To screen for small molecule inhibitors of ATM kinase activity, an in vitro kinase assay is adapted, and an ELISA assay develops which measured the phosphorylation status of the ATM downstream target p53. Recombinant GST-p53(1-101) and full-length Flag-tagged ATM & ATR are purified for use in the ELISA and in vitro kinase assays. Briefly, Nunc 96 well Maxisorp plates are coated overnight (4 °C) with 2μg of purified, recombinant GST-p53(1-101) in PBS. All subsequent incubations are performed at room temperature. The plates are washed (0.05%v/v-Tween/PBS) before addition of purified recombinant full-length ATM kinase (30 ng–60 ng) in a final volume of 80μL of reaction buffer (20 mM HEPES, 50 mM NaCl, 10 mM MgCl2, 10 mM MnCl2, 1 mM DTT and 1 μM ATP) in the presence or absence of CP-466722. CP-466722 (10 μM) is added to plates in duplicate and the kinase assay is incubated (90 minutes). Plates are washed (0.05%v/v-Tween/PBS), blocked (1hour, 1%w/v-BSA/PBS) and rinsed before anti-Phospho(Ser15)-p53 antibody (1:1000/PBS) is added to the plates and incubated (1hour). To reduce non-specific binding plates are washed (0.05%v/v-Tween/PBS) prior to incubation (1hour) with HRP-conjugated goat anti-rabbit IgG secondary antibody (1:5000/PBS). Secondary antibody that is linked to the phosphorylated GST-p53(1–101) protein is detected with TMB substrate reagent. Plates are developed (15 minutes–30 minutes) and the reaction is stopped (1 M H2SO4 final concentration) before absorbance is determined (λ450 nM). CP-466722 that inhibits ATM kinase activity in ELISA assays, are characterized with respect to inhibition of ATM/ATR kinases using in vitro kinase assays. Western blotting using the anti-Phospho(Ser15)-p53 antibody is used as a readout of ATM/ATR inhibition. Extended analysis of CP466722 (10 μM) against a commercially available panel of kinases is performed by Upstate.
Cell Research	HeLa or A-T (GM02052 expressing hTERT) cells are plated in triplicate and incubated for 24 hours. Cells are pre-treated: DMSO, CP466722 or KU55933 prior to IR (0-10 gy). Cells are incubated for 4 hours following IR before media is removed, cells washed (PBS), trypsined, counted and re-plated (2000 cells/plate, 10 cm plates) in the absence of drug and incubated for 10 days. Prior to colony counting, cells are washed (PBS), stained (PBS, 0.0037%v/v-formaldehyde, 0.1%w/v-crystal violet), rinsed (dWater) and dried. Defined populations (>50 cells) are counted as one surviving colony, data are calculated as percentage surviving colonies relative to control plates +/− SE. (Only for Reference)

Synonyms	CP 466722, CP466722
Molecular Weight	349.35
Formula	C17H15N7O2
CAS No.	1080622-86-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7 mg/mL (20.04 mM), Sonification is recommended.

References and Literature

1. Rainey MD, et al. Cancer Res, 2008, 68(18), 7466-7474. 2. Guo K, et al. J Biomol Screen. 2014, 19(4), 538-546.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Obesity Compound Library Neural Regeneration Compound Library Antidepressant Compound Library Anti-Cancer Metabolism Compound Library Cancer Cell Differentiation Compound Library Anti-Breast Cancer Compound Library PI3K-AKT-mTOR Compound Library Anti-Ovarian Cancer Compound Library

Related Products

Related compounds with same targets

CGK733 ATM Inhibitor-8 KU-55933 ETP-46464 (Z)-Mirin AZ32 Tuvusertib Gartisertib

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Keywords

CP-466722 1080622-86-1 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR ATM and RAD3 related Inhibitor CP 466722 Ataxia telangiectasia mutated CP466722 inhibit inhibitor

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