Ceralasertib (AZD6738)

Catalog No.S7693 Batch:S769305

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Technical Data

Formula

C20H24N6O2S
Molecular Weight 412.51 CAS No. 1352226-88-0
Solubility (25°C)* In vitro DMSO 83 mg/mL (201.2 mM)
Ethanol 83 mg/mL (201.2 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
1.88mg/ml Taking the 1 mL working solution as an example, add 50 μL of 37.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
Targets
ATR [1]
(Cell-free assay)
1 nM
In vitro

In four Kras mutant cell lines: H23, H460, A549, and H358, AZD6738 inhibits ATR kinase activity and impairs cell viability. In ATM-deficient H23 cells, AZD6738 strongly synergizes with NSC 119875 to induce rapid cell death. [1] In p53 or ATM defective cells, AZD6738 treatment results in replication fork stalls and accumulation of unrepaired DNA damage, resulting in cell death by mitotic catastrophe. [2]
In vivo

In nude mice bearing H460 and H23 tumors, AZD6738 (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and the the combination with NSC 119875 causes rapid regression of ATM-deficient H23 tumors. [1] In nude mice bearing LoVo xenografts, a combination of AZD6738 (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy. [3]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    H23, H460, A549, and H358 cells

  • Concentrations

    ~30 μM

  • Incubation Time

    48 h

  • Method

    Cells are treated in white walled, clear bottom 96-well plates with the indicated doses of AZD6738, NSC 119875, LY-188011, or combination for 48 h. ATP levels are assessed as surrogate measure of viability is assessed using the CellTiter-Glo Luminescent Cell Viability Assay and Safire2 plate reader. Raw data are corrected for background luminescence prior to further analysis. For AZD6738 treatment, log dose response curves are generated in GraphPad Prism 6 by nonlinear regression (log(inhibitor) vs. response with variable slope) of log-transformed (x = log(x)) data normalized to the mean of untreated controls. GI50 values, defined as the dose X at which Y = 50%, were extrapolated from dose response curves.
Animal Study:

[1]
  • Animal Models

    Female athymic nude mice bearing H23 or H460 xenografts

  • Dosages

    25 or 50 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1346]

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2018, 37(1):205]

Data from [Data independently produced by , , Sci Rep, 2017, 7:41950]

Data from [Data independently produced by , , J Dermatol Sci, 2016, 84(3):239-247]

Selleck's Ceralasertib (AZD6738) has been cited by 116 publications

Deregulated DNA ADP-ribosylation impairs telomere replication [ Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01279-6] PubMed: 38714889
H2AX promotes replication fork degradation and chemosensitivity in BRCA-deficient tumours [ Nat Commun, 2024, 15(1):4430] PubMed: 38789420
Functionally-instructed modifiers of response to ATR inhibition in experimental glioma [ J Exp Clin Cancer Res, 2024, 43(1):77] PubMed: 38475864
Loss of POLE3-POLE4 unleashes replicative gap accumulation upon treatment with PARP inhibitors [ Cell Rep, 2024, 43(5):114205] PubMed: 38753485
ATR inhibition radiosensitizes cells through augmented DNA Damage and G2 cell cycle arrest abrogation [ JCI Insight, 2024, e179599] PubMed: 39235982
KRASG 12C-inhibitor-based combination therapies for pancreatic cancer: insights from drug screening [ Mol Oncol, 2024, 10.1002/1878-0261.13725] PubMed: 39253995
Diffusion of activated ATM explains γH2AX and MDC1 spread beyond the DNA damage site [ iScience, 2024, 27(9):110826] PubMed: 39310780
Ruthenium drug BOLD-100 regulates BRAFMT colorectal cancer cell apoptosis through AhR/ROS/ATR signaling axis modulation [ Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151] PubMed: 39083088
Afatinib or Bevacizumab in combination with Osimertinib efficiently control tumor development in orthotopic murine models of non-small lung cancer [ PLoS One, 2024, 19(6):e0304914] PubMed: 38935790
ATR inhibition activates cancer cell cGAS/STING-interferon signaling and promotes antitumor immunity in small-cell lung cancer [ Sci Adv, 2024, 10(39):eado4618] PubMed: 39331709

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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