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

Ceralasertib (Synonyms: AZD6738)

Cat. No.: HY-19323 Purity: 99.76%
Handling Instructions

Ceralasertib (AZD6738) is a potent 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
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
100 mg USD 888 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Publications Citing Use of MCE Ceralasertib

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Description

Ceralasertib (AZD6738) is a potent 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 cisplatin and gemcitabine in NSCLC cell lines with intact ATM kinase signaling, and potently synergizes with cisplatin 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].

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 cisplatin in xenograft models. Remarkably, the combination of cisplatin and Ceralasertib (AZD6738) resolves ATM-deficient lung cancer xenografts[1].

Clinical Trial
Molecular Weight

412.51

Formula

C₂₀H₂₄N₆O₂S

CAS No.

1352226-88-0

SMILES

O=[[email protected]@](C1(CC1)C2=NC(C3=C4C(NC=C4)=NC=C3)=NC(N5CCOC[[email protected]]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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 38 mg/mL (92.12 mM)

*"≥" means soluble, but saturation unknown.

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:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    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

  • 3.

    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 provided by MCE.
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

Purity: 99.76%

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Ceralasertib
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