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860352-01-8,MFCD12406007
Catalog No.:AA00GRRV

860352-01-8 | Azd7762

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1mg
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$15.00   $11.00
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10mg
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00GRRV
Chemical Name:
Azd7762
CAS Number:
860352-01-8
Molecular Formula:
C17H19FN4O2S
Molecular Weight:
362.4218
MDL Number:
MFCD12406007
SMILES:
NC(=O)Nc1cc(sc1C(=O)N[C@H]1CCCNC1)c1cccc(c1)F
Properties
Computed Properties
 
Complexity:
495  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
25  
Hydrogen Bond Acceptor Count:
5  
Hydrogen Bond Donor Count:
4  
Rotatable Bond Count:
4  
XLogP3:
2.3  

Downstream Synthesis Route

[1]CurrentPatentAssignee:ASTRAZENECAPLC-WO2009/133389,2009,A1Locationinpatent:Page/Pagecolumn29

[2]Ball,Matthew;Jones,MartinF.;Kenley,Fiona;Pittam,J.David[OrganicProcessResearchandDevelopment,2017,vol.21,#3,p.310-316]

[3]CurrentPatentAssignee:JANETKAJAMESWALTER;ASTRAZENECAPLC-WO2005/66163,2005,A2Locationinpatent:Page/Pagecolumn67

[1]CurrentPatentAssignee:ASTRAZENECAPLC-WO2009/133389,2009,A1Locationinpatent:Page/Pagecolumn30-31

[1]CurrentPatentAssignee:ASTRAZENECAPLC-WO2009/133389,2009,A1Locationinpatent:Page/Pagecolumn31-32

[1]Ball,Matthew;Jones,MartinF.;Kenley,Fiona;Pittam,J.David[OrganicProcessResearchandDevelopment,2017,vol.21,#3,p.310-316]

Literature

Title: Cellular impedance assays for predictive preclinical drug screening of kinase inhibitor cardiovascular toxicity.

Journal: Toxicological sciences : an official journal of the Society of Toxicology 20131001

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: The checkpoint kinase inhibitor AZD7762 potentiates chemotherapy-induced apoptosis of p53-mutated multiple myeloma cells.

Journal: Molecular cancer therapeutics 20120801

Title: Synthesis and biological evaluation of analogs of the marine alkaloids granulatimide and isogranulatimide.

Journal: European journal of medicinal chemistry 20120801

Title: Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.

Journal: Journal of medicinal chemistry 20120614

Title: Forced mitotic entry of S-phase cells as a therapeutic strategy induced by inhibition of WEE1.

Journal: Cancer discovery 20120601

Title: Chk'ing p53-deficient breast cancers.

Journal: The Journal of clinical investigation 20120402

Title: Targeting Chk1 in p53-deficient triple-negative breast cancer is therapeutically beneficial in human-in-mouse tumor models.

Journal: The Journal of clinical investigation 20120402

Title: Evaluation of checkpoint kinase targeting therapy in acute myeloid leukemia with complex karyotype.

Journal: Cancer biology & therapy 20120301

Title: Potentiation of the novel topoisomerase I inhibitor indenoisoquinoline LMP-400 by the cell checkpoint and Chk1-Chk2 inhibitor AZD7762.

Journal: Cancer research 20120215

Title: Selective radiosensitization of p53 mutant pancreatic cancer cells by combined inhibition of Chk1 and PARP1.

Journal: Cell cycle (Georgetown, Tex.) 20111215

Title: Cytokinetically quiescent (G0/G1) human multiple myeloma cells are susceptible to simultaneous inhibition of Chk1 and MEK1/2.

Journal: Blood 20111110

Title: Checkpoint kinase inhibitor synergizes with DNA-damaging agents in G1 checkpoint-defective neuroblastoma.

Journal: International journal of cancer 20111015

Title: Chk2 deficiency in Myc overexpressing lymphoma cells elicits a synergistic lethal response in combination with PARP inhibition.

Journal: Cell cycle (Georgetown, Tex.) 20111015

Title: Ataxia telangiectasia mutated- and Rad3-related kinase drives both the early and the late DNA-damage response to the monofunctional antitumour alkylator S23906.

Journal: The Biochemical journal 20110701

Title: Assessment of chk1 phosphorylation as a pharmacodynamic biomarker of chk1 inhibition.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110601

Title: Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.

Journal: Journal of medicinal chemistry 20110414

Title: Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR.

Journal: Nature chemical biology 20110413

Title: Inhibition of checkpoint kinase 1 sensitizes lung cancer brain metastases to radiotherapy.

Journal: Biochemical and biophysical research communications 20110304

Title: Bayesian hierarchical changepoint methods in modeling the tumor growth profiles in xenograft experiments.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110301

Title: Structure-specific DNA endonuclease Mus81/Eme1 generates DNA damage caused by Chk1 inactivation.

Journal: PloS one 20110101

Title: Poly(ADP-ribose) polymerase 1 modulates the lethality of CHK1 inhibitors in carcinoma cells.

Journal: Molecular pharmacology 20101101

Title: Preclinical pharmacokinetic/pharmacodynamic models to predict synergistic effects of co-administered anti-cancer agents.

Journal: Cancer chemotherapy and pharmacology 20100701

Title: Structure-based and shape-complemented pharmacophore modeling for the discovery of novel checkpoint kinase 1 inhibitors.

Journal: Journal of molecular modeling 20100701

Title: Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair.

Journal: Cancer research 20100615

Title: In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20100401

Title: Targeting Chk1 in the replicative stress response.

Journal: Cell cycle (Georgetown, Tex.) 20100315

Title: Chk1 inhibition after replicative stress activates a double strand break response mediated by ATM and DNA-dependent protein kinase.

Journal: Cell cycle (Georgetown, Tex.) 20100301

Title: Cell cycle kinases as therapeutic targets for cancer.

Journal: Nature reviews. Drug discovery 20090701

Title: AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.

Journal: Molecular cancer therapeutics 20080901

Title: Zabludoff SD, et al. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol Cancer Ther. 2008 Sep;7(9):2955-66.

Title: Quin J, et al. Inhibition of RNA polymerase I transcription initiation by CX-5461 activates non-canonical ATM/ATR signaling. Oncotarget. 2016 Aug 2;7(31):49800-49818.

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