2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. Ceralasertib

Ceralasertib  (Synonyms: AZD6738)

Cat. No.: HY-19323 Purity: 99.00%
COA Handling Instructions

Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.

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

Ceralasertib Chemical Structure

Ceralasertib Chemical Structure

CAS No. : 1352226-88-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 180 In-stock
50 mg USD 528 In-stock
100 mg USD 888 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Ceralasertib:

Ceralasertib Related Antibodies

Top Publications Citing Use of Products

    Ceralasertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Nov 16;41(1):323.  [Abstract]

    Ceralasertib (AZD6738; 1, 2 µM) signifcantly decreases the protein levels of ATR, IFI16 and HuR in a dose-dependent manner in GSC 267 and GSC 20 cells.

    View All ATM/ATR Isoform Specific Products:

    View All Isoforms
    ATM ATR

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.

    IC50 & Target[1]

    ATR

    1 nM (IC50)

    PI3Kδ

    6.8 μM (IC50)

    DYRK

    10.8 μM (IC50)

    In Vitro

    Ceralasertib (AZD6738) is a potent inhibitor of ATR kinase activity with an IC50 of 0.001 μM against the isolated enzyme and 0.074 μM against ATR kinase-dependent CHK1 phosphorylation in cells. Ceralasertib (AZD6738) induces cell death and senescence in non-small cell lung cancer (NSCLC) cell lines. Ceralasertib (AZD6738) impairs viability of four Kras mutant cell lines: H23, H460, A549, and H358. , with the lowest GI50 and greatest maximal inhibition in H460 and H23 cells (1.05 μM, 88.0% and 2.38 μM, 86.2%, respectively). Ceralasertib (AZD6738) potentiates the cytotoxicity of CDDP and NSC 613327 in NSCLC cell lines with intact ATM kinase signaling, and potently synergizes with CDDP in ATM-deficient NSCLC cells[1]. Ceralasertib (AZD6738) inhibits human breast cancer cell lines with IC50 values less than 1 μM using MTT assay. Ceralasertib (AZD6738) induces cell cycle arrest and apoptosis. It downregulates DNA damage response molecules and cell proliferative signaling molecules[2].

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

    Ceralasertib Related Antibodies
    In Vivo

    Daily administration of Ceralasertib (AZD6738) and ATR kinase inhibition for 14 consecutive days is tolerated in mice and enhances the therapeutic efficacy of CDDP in xenograft models. Remarkably, the combination of CDDP and Ceralasertib (AZD6738) resolves ATM-deficient lung cancer xenografts[1].

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

    412.51

    Appearance

    Solid

    Formula

    C20H24N6O2S
    CAS No.
    SMILES

    O=[S@@](C1(CC1)C2=NC(C3=C4C(NC=C4)=NC=C3)=NC(N5CCOC[C@H]5C)=C2)(C)=N
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (303.02 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4242 mL 12.1209 mL 24.2418 mL
    5 mM 0.4848 mL 2.4242 mL 4.8484 mL
    10 mM 0.2424 mL 1.2121 mL 2.4242 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (24.24 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 6.67 mg/mL (16.17 mM); Clear solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.76%

    COA (253 KB) HNMR (195 KB) LCMS (467 KB) Elemental Analysis Report (111 KB)

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

    Ceralasertib (AZD6738) is dissolved in DMSO at 30 mM and diluted in DMSO to desired working concentrations. The final DMSO concentration in media for all conditions and controls is 0.1% for Ceralasertib (AZD6738) dose response experiments, 0.05% for Ceralasertib (AZD6738) + chemotherapy viability experiments, and 0.025% for all experiments involving 0.3 μM and 1.0 μM doses of Ceralasertib (AZD6738)[1].

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

    Mice[1]
    Ceralasertib (AZD6738) is dissolved in DMSO at a concentration of 25 mg/mL or 50 mg/mL and diluted 1:5 in propylene glycol. Ceralasertib (AZD6738) is administered by oral gavage at 25 mg/kg (H23) or 50 mg/kg (H460) for 14 consecutive days. The dosing volume is 10 mL/kg.[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Ceralasertib 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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Ceralasertib1352226-88-0AZD6738AZD 6738AZD-6738ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Ceralasertib
    Cat. No.:
    HY-19323
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.