2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. CP-466722

CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 0.41 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.

For research use only. We do not sell to patients.

CP-466722 Chemical Structure

CP-466722 Chemical Structure

CAS No. : 1080622-86-1

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1 mg USD 35 In-stock
5 mg USD 88 In-stock
10 mg USD 154 In-stock
50 mg USD 418 In-stock
100 mg USD 682 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

CP-466722 Related Antibodies

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ATM ATR

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  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 0.41 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.

IC50 & Target[2]

ATM

4.1 μM (IC50)

In Vitro

CP-466722 (CP466722, 6-10 μM) inhibits IR-induced ATM kinase activity, and the inhibition can be rapidly and completely reversed. CP466722 (6, 10 μM) inhibits p53 induction and ATM-dependent phosphorylation in mouse cells, but CP466722 fails to inhibit ATR activity and ATR-dependent phosphorylation of Chk1. CP466722 (6 μM) disrupts ATM-dependent cell cycle checkpoints in cells[1]. CP466722 (1 μM) completely inhibits ATM-dependent phosphorylation in MCF7 cells. CP466722 (10 μM) reduces pKAP1 phosphorylation in MCF7 cells, with an IC50 of 0.41 μM. CP466722 (10 μM) inhibits both pATM and pKAP1 signals[2]. CP-466722 (CP466722, 5-50 μM) inhibits proliferation of SKBr-3 cancer cells more strongly than MCF-7 cancer cells. CP466722 (10 μM) also slightly increases proportions of MCF-7 and SKBr-3 cells in the G1 phase after treatment for 48 hours[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CP-466722 Related Antibodies
Molecular Weight

349.35

Formula

C17H15N7O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(C2=NC=CC=C2)=NN1C3=C4C=C(OC)C(OC)=CC4=NC=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 1 mg/mL (2.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8625 mL 14.3123 mL 28.6246 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.91%

COA (258 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

To screen for small molecule inhibitors of ATM kinase activity, an in vitro kinase assay is carried out, and an ELISA assay developes which measures 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 2 μg 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 (30-60 ng) in a final volume of 80 μL of reaction buffer (20 mM HEPES, 50 mM NaCl2, 10 mM MgCl2, 10 mM MnCl2, 1 mM DTT and 1 μM ATP) in the presence or absence of compound. Compounds including CP-466722 (10 μM) are added to plates in duplicate and the kinase assay is incubated (90 min). Plates are washed (0.05% v/v-Tween/PBS), blocked (1 h, 1% w/v-BSA/PBS) and rinsed before anti-Phospho(Ser15)-p53 antibody (1:1000/PBS) is added to the plates and incubated (1 h). To reduce non-specific binding plates are washed (0.05% v/v-Tween/PBS) prior to incubation (1 h) 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 (15-30 min) and the reaction is stopped (1M H2SO4 final concentration) before absorbance is determined (λ450 nm). Compounds that inhibit 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are plated in triplicate (40,000 cells/plate), incubated as required before culture media and trypsinsed cells are combined and viability determined: Vi-CELL™ XR cell viability analyzer[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* 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 2.8625 mL 14.3123 mL 28.6246 mL 71.5615 mL
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CP-466722 Related Classifications

Help & FAQs
  • 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:

CP-4667221080622-86-1CP466722CP 466722ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

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