Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H24N6O2S |
Molecular Weight | 412.509 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H]1COCCN1C2=NC(=NC(=C2)C3(CC3)[S@](C)(=N)=O)C4=CN=CC5=C4C=CN5
InChI
InChIKey=DTTJKLNXNZAVSM-JYCIKRDWSA-N
InChI=1S/C20H24N6O2S/c1-13-12-28-8-7-26(13)18-9-17(20(4-5-20)29(2,21)27)24-19(25-18)15-10-22-11-16-14(15)3-6-23-16/h3,6,9-11,13,21,23H,4-5,7-8,12H2,1-2H3/t13-,29-/m1/s1
Ceralasertib, previously known as AZD6738, a potent and selective inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase was developed as an anticancer agent. Prevention of ATR-mediated signaling leads to the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. AZD6738 as a combination therapy participates in phase II clinical trials for the treatment of gastric adenocarcinoma and malignant melanoma (in combination with durvalumab). For the treatment of gastric and breast cancer in combination with carboplatin, or with olaparib or with MEDI4736. Combination of acalabrutinib and AZ6738 is used in phase II trials for patients with chronic lymphocytic Leukemia. Besides, AZD6738 participates in umbrella Phase II study in patients with metastatic non-small cell lung cancer (NSCLC) who have progressed on an anti-programmed cell death-1/anti-programmed cell death ligand 1 (anti-PD-1/PD-L1) containing therapy.
Originator
Approval Year
PubMed
Title | Date | PubMed |
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The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of cisplatin to resolve ATM-deficient non-small cell lung cancer in vivo. | 2015 Dec 29 |
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AZD6738, A Novel Oral Inhibitor of ATR, Induces Synthetic Lethality with ATM Deficiency in Gastric Cancer Cells. | 2017 Apr |
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Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. | 2018 Nov 21 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT03780608
AZD6738 will be administered at 240 mg twice daily on days 1 to 7 in Cycle 0 (lead-in period) and therafter at 240 mg BD on days 22 to 28 in a 28-day cycle.
Route of Administration:
Oral
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NCI_THESAURUS |
C155926
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NCI_THESAURUS |
C129825
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100000175302
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HI-87
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85RE35306Z
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C111993
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DB14917
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CHEMBL3545178
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121596701
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ACTIVE MOIETY