860352-01-8 | Azd7762

Packsize	Purity	Availability	Price	Discounted Price
1mg	98+%	in stock	$14.00	$10.00
10mg	98+%	in stock	$51.00	$36.00

Description

• Catalog Number: AH82391
• 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

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

Literature

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

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

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

  Bioorganic & medicinal chemistry letters 20130801

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

  Molecular cancer therapeutics 20120801

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

  European journal of medicinal chemistry 20120801

• 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 of medicinal chemistry 20120614

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

  Cancer discovery 20120601

• Chk'ing p53-deficient breast cancers.

  The Journal of clinical investigation 20120402

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

  The Journal of clinical investigation 20120402

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

  Cancer biology & therapy 20120301

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

  Cancer research 20120215

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

  Cell cycle (Georgetown, Tex.) 20111215

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

  Blood 20111110

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

  International journal of cancer 20111015

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

  Cell cycle (Georgetown, Tex.) 20111015

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

  The Biochemical journal 20110701

• Assessment of chk1 phosphorylation as a pharmacodynamic biomarker of chk1 inhibition.

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

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

  Journal of medicinal chemistry 20110414

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

  Nature chemical biology 20110413

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

  Biochemical and biophysical research communications 20110304

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

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

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

  PloS one 20110101

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

  Molecular pharmacology 20101101

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

  Cancer chemotherapy and pharmacology 20100701

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

  Journal of molecular modeling 20100701

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

  Cancer research 20100615

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

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

• Targeting Chk1 in the replicative stress response.

  Cell cycle (Georgetown, Tex.) 20100315

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

  Cell cycle (Georgetown, Tex.) 20100301

• Cell cycle kinases as therapeutic targets for cancer.

  Nature reviews. Drug discovery 20090701

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

  Molecular cancer therapeutics 20080901