761439-42-3 | Nvp-tae684

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$48.00	$34.00
10mg	95%	in stock	$115.00	$81.00
25mg	95%	in stock	$194.00	$136.00
50mg	95%	in stock	$306.00	$214.00
100mg	95%	in stock	$507.00	$355.00
250mg	95%	in stock	$869.00	$609.00

Description

• Catalog Number: AH51099
• Chemical Name: Nvp-tae684
• CAS Number: 761439-42-3
• Molecular Formula: C30H40ClN7O3S
• Molecular Weight: 614.2017
• MDL Number: MFCD11977634
• SMILES: COc1cc(ccc1Nc1ncc(c(n1)Nc1ccccc1S(=O)(=O)C(C)C)Cl)N1CCC(CC1)N1CCN(CC1)C

Computed Properties

• Complexity: 940
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 42
• Hydrogen Bond Acceptor Count: 10
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 9
• XLogP3: 5.7

Literature

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  Journal of medicinal chemistry 20160526

• Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.

  Journal of medicinal chemistry 20131024

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

  Bioorganic & medicinal chemistry letters 20130801

• Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.

  Journal of medicinal chemistry 20130725

• Anaplastic Lymphoma Kinase (ALK) regulates initiation of transcription of MYCN in neuroblastoma cells.

  Oncogene 20121213

• Activation of HER family signaling as a mechanism of acquired resistance to ALK inhibitors in EML4-ALK-positive non-small cell lung cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20121115

• Differential protein stability and ALK inhibitor sensitivity of EML4-ALK fusion variants.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120901

• Paracrine receptor activation by microenvironment triggers bypass survival signals and ALK inhibitor resistance in EML4-ALK lung cancer cells.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120701

• Development of treatment strategies for advanced neuroblastoma.

  International journal of clinical oncology 20120601

• Small-molecule inhibitors of the c-Fes protein-tyrosine kinase.

  Chemistry & biology 20120420

• Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

  Bioorganic & medicinal chemistry letters 20120301

• Activating ALK mutations found in neuroblastoma are inhibited by Crizotinib and NVP-TAE684.

  The Biochemical journal 20111215

• ALK mutations conferring differential resistance to structurally diverse ALK inhibitors.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20111201

• Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen.

  Chemical biology & drug design 20111201

• Comprehensive analysis of kinase inhibitor selectivity.

  Nature biotechnology 20111030

• Anaplastic lymphoma kinase (ALK) inhibitor response in neuroblastoma is highly correlated with ALK mutation status, ALK mRNA and protein levels.

  Cellular oncology (Dordrecht) 20111001

• A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors.

  Cancer research 20110915

• Stimulation of the midkine/ALK axis renders glioma cells resistant to cannabinoid antitumoral action.

  Cell death and differentiation 20110601

• Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK.

  Proceedings of the National Academy of Sciences of the United States of America 20110503

• Targeting oncogenic ALK: a promising strategy for cancer treatment.

  Molecular cancer therapeutics 20110401

• Inhibition of anaplastic lymphoma kinase (ALK) activity provides a therapeutic approach for CLTC-ALK-positive human diffuse large B cell lymphomas.

  PloS one 20110101

• Anaplastic Lymphoma Kinase: role in specific tumours, and development of small molecule inhibitors for cancer therapy.

  Cancer letters 20101228

• The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers.

  Cancer research 20101215

• Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.

  Chemistry & biology 20101124

• Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors.

  Biochemistry 20100817

• Anaplastic lymphoma kinase activates the small GTPase Rap1 via the Rap1-specific GEF C3G in both neuroblastoma and PC12 cells.

  Oncogene 20100513

• Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors.

  Cancer research 20080501

• Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.

  Proceedings of the National Academy of Sciences of the United States of America 20070102