Molecular Weight(MW): 412.51
AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
Cited by 6 Publications
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. In ATM-deficient H23 cells, AZD6738 strongly synergizes with cisplatin to induce rapid cell death.  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. 
|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 cisplatin causes rapid regression of ATM-deficient H23 tumors.  In nude mice bearing LoVo xenografts, a combination of AZD6738 (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy. |
|Animal Research: ||
|In vitro||DMSO||82 mg/mL (198.78 mM)|
|Ethanol||41 mg/mL warmed (99.39 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10% DMSO+40% propylene glycol+ddH2O
For best results, use promptly after mixing.
* 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.
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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).
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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|
|NCT03669601||Not yet recruiting||Cancer||CCTU- Cancer Theme|AstraZeneca|Cambridge University Hospitals NHS Foundation Trust||March 31 2019||Phase 1|
|NCT03740893||Not yet recruiting||Breast Neoplasm||Institute of Cancer Research United Kingdom|AstraZeneca||February 2019||Phase 2|
|NCT03682289||Not yet recruiting||Clear Cell Renal Cell Carcinoma|Locally Advance Pancreatic Ductal Adenocarcinoma|Locally Advanced Malignant Solid Neoplasm|Metastatic Malignant Solid Neoplasm|Metastatic Renal Cell Carcinoma|Metastatic Urothelial Carcinoma|Pancreatic Ductal Adenocarcinoma|Stage III Pancreatic Cancer AJCC v8|Stage III Renal Cell Cancer AJCC v8|Stage IV Pancreatic Cancer AJCC v8|Stage IV Renal Cell Cancer AJCC v8||University of California San Francisco||December 1 2018||Phase 2|
|NCT03527147||Recruiting||NHL|DLBCL|Non-hodgkin''s Lymphoma|Diffuse Large B Cell Lymphoma||Acerta Pharma BV|AstraZeneca||June 19 2018||Phase 1|
|NCT03428607||Not yet recruiting||SCLC||Samsung Medical Center||February 2018||Phase 2|
|NCT03330847||Recruiting||Metastatic Triple Negative Breast Cancer||AstraZeneca||February 21 2018||Phase 2|
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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