AZD6738

Catalog No.S7693

AZD6738 Chemical Structure

Molecular Weight(MW): 412.51

AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.

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2 Customer Reviews

  • AZD6738 (AZD) synergizes with cytarabine (ara-C) to induce apoptosis and proliferation inhibition in AML cells. (a) OCI-AML3 cells were treated with cytarabine and AZD6738, alone or in combination, for 24 h and then subjected to annexin V-FITC/PI staining and flow cytometry analyses. CI values were calculated using CompuSyn software. Combined drug treatments were compared to single drug treatment using 1-way ANOVA with Bonferroni post hoc test. ***indicates p < 0.001. (b and c) OCI-AML3 cells were treated with cytarabine and AZD-6738, alone or in combination, for 24 h. Whole cell lysates were subjected to Western blotting and probed with the indicated antibodies.

    Sci Rep, 2017, 7:41950. AZD6738 purchased from Selleck.

    MyLa2000 cells were irradiated with UVA at dose 1.6 J/cm2. Kinase inhibitors were added at the following concentrations: 10 μM VE-821, 1 μM VE-822, 1.6 μM Chir-124, 1 μM AZD6738, 1 μM MK8776 (selected basing on toxicity studies performed previously; data not shown) 30 minutes before irradiation (30 min before UVA), immediately before irradiation (0 min before UVA) or immediately after irradiation (0 min after UVA). Cell viability was analyzed 48 hours after treatment by PI exclusion assay.

    J Dermatol Sci, 2016, 84(3):239-247. AZD6738 purchased from Selleck.

Purity & Quality Control

Choose Selective ATM/ATR Inhibitors

Biological Activity

Description 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. AZD6738 strongly synergizes with cisplatin in an ATM-deficient NSCLC cell line in vitro[1]. In p53 or ATM defective cells, AZD6738 treatment resulted in replication fork stalls and accumulation of unrepaired DNA damage, as evidenced by γH2AX and 53BP1 foci formation, which was carried through into mitosis, resulting in cell death by mitotic catastrophe[2].

In vivo The combination of 50 mg/kg AZD6738 and cisplatin resulted in a 75.5% mean tumor growth inhibition (TGI) of H460 xenografts at day 14 (P ≤ 0.0001 compared to vehicle). Growth of tumors treated with the combination was also significantly different from that of tumors treated with cisplatin or AZD6738 alone [1]. In LoVo derived mouse xenograft, a combination of AZD6738 (50 mg/kg) + IR (2 Gy) can be adjusted to avoid toxicity while still maintaining efficacy[3].

Protocol

Cell Research:

[1]

+ Expand
  • 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, cisplatin, gemcitabine, or combination for 48 h. ATP levels are assessed as surrogate measure of viability was 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. 


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female athymic nude (Foxn1nu) mice
  • Formulation: 10% DMSO, 40% propylene glycol, and 50% sterile dH2O
  • Dosages: 25 or 50 mg/kg
  • Administration: p.o
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (198.78 mM)
Ethanol 41 mg/mL warmed (99.39 mM)
Water Insoluble
In vivo Add solvents individually and in order:
10% DMSO+40% propylene glycol+ddH2O
10mg/mL

* 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.

Chemical Information

Molecular Weight 412.51
Formula

C20H24N6O2S

CAS No. 1352226-88-0
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03022409 Not yet recruiting Head and Neck Squamous Cell Carcinoma AstraZeneca March 2017 Phase 1
NCT02630199 Recruiting Refractory Cancer Samsung Medical Center December 2015 Phase 1
NCT02264678 Recruiting Advanced Solid Malignancies, Head and Neck Squamous Cell Carinoma, and ATM Deficient NSCLC Adenocarcinoma, Gastric Cancer and Gastro-oesophageal Junction AstraZeneca October 2014 Phase 1
NCT02223923 Recruiting Solid Tumour Refractory to Conventional Treatment Royal Marsden NHS Foundation Trust|AstraZeneca|Cancer Research UK|RM/ICR Biomedical Research Centre July 2014 Phase 1
NCT01955668 Completed 11q-deleted Relapsed/Refractory Chronic Lymphocytic Leukaemia (CLL),|Prolymphocytic Leukaemia (PLL)|B Cell Lymphomas AstraZeneca|CLL Consortium November 2013 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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ATM/ATR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID