Molecular Weight(MW): 412.51
AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
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
|Description||AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.|
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. 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.
|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 . 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.|
|In vitro||DMSO||82 mg/mL (198.78 mM)|
|Ethanol||41 mg/mL warmed (99.39 mM)|
|In vivo||Add solvents individually and in order:
10% DMSO+40% propylene glycol+ddH2O
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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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