796967-16-3 | Linifanib

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$52.00	$36.00
5mg	95%	in stock	$128.00	$90.00
10mg	95%	in stock	$179.00	$126.00
100mg	95%	in stock	$212.00	$149.00
250mg	95%	in stock	$339.00	$237.00
1g	95%	in stock	$993.00	$695.00

Description

• Catalog Number: AB48185
• Chemical Name: Linifanib
• CAS Number: 796967-16-3
• Molecular Formula: C21H18FN5O
• Molecular Weight: 375.3989
• MDL Number: MFCD11840918
• SMILES: O=C(Nc1cc(C)ccc1F)Nc1ccc(cc1)c1cccc2c1c(N)n[nH]2

Computed Properties

• Complexity: 541
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 28
• Hydrogen Bond Acceptor Count: 4
• Hydrogen Bond Donor Count: 4
• Rotatable Bond Count: 3
• XLogP3: 3.9

Literature

• A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

  Nature chemical biology 20151201

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

  Bioorganic & medicinal chemistry letters 20130801

• Phase 1 trial of linifanib (ABT-869) in patients with refractory or relapsed acute myeloid leukemia.

  Leukemia & lymphoma 20120801

• 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).

  Bioorganic & medicinal chemistry letters 20120715

• FDG-PET as a pharmacodynamic biomarker for early assessment of treatment response to linifanib (ABT-869) in a non-small cell lung cancer xenograft model.

  Cancer chemotherapy and pharmacology 20120601

• An open-label, phase 1 study evaluating safety, tolerability, and pharmacokinetics of linifanib (ABT-869) in Japanese patients with solid tumors.

  Cancer chemotherapy and pharmacology 20120601

• A novel multi-targeted tyrosine kinase inhibitor, linifanib (ABT-869), produces functional and structural changes in tumor vasculature in an orthotopic rat glioma model.

  Cancer chemotherapy and pharmacology 20120401

• BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML.

  British journal of cancer 20120131

• Phase 2 trial of linifanib (ABT-869) in patients with advanced renal cell cancer after sunitinib failure.

  European journal of cancer (Oxford, England : 1990) 20111201

• A comparative study of dynamic contrast-enhanced MRI parameters as biomarkers for anti-angiogenic drug therapy.

  NMR in biomedicine 20111101

• Comprehensive analysis of kinase inhibitor selectivity.

  Nature biotechnology 20111030

• Phase 2 trial of Linifanib (ABT-869) in patients with advanced non-small cell lung cancer.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20110801

• Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).

  Bioorganic & medicinal chemistry 20110715

• ABT-869, a multitargeted receptor tyrosine kinase inhibitor, reduces tumor microvascularity and improves vascular wall integrity in preclinical tumor models.

  The Journal of pharmacology and experimental therapeutics 20110701

• Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.

  European journal of medicinal chemistry 20110601

• The multitargeted receptor tyrosine kinase inhibitor linifanib (ABT-869) induces apoptosis through an Akt and glycogen synthase kinase 3β-dependent pathway.

  Molecular cancer therapeutics 20110601

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

  Chemistry & biology 20101124

• Antiangiogenic agents in advanced gastrointestinal malignancies: past, present and a novel future.

  Oncotarget 20101101

• Linifanib.

  Drugs in R&D 20100701

• ABT-869 inhibits the proliferation of Ewing Sarcoma cells and suppresses platelet-derived growth factor receptor beta and c-KIT signaling pathways.

  Molecular cancer therapeutics 20100301

• Three dimensional pharmacophore modelling for c-Kit receptor tyrosine kinase inhibitors.

  European journal of medicinal chemistry 20100101

• Pulse-modulated second harmonic imaging microscope quantitatively demonstrates marked increase of collagen in tumor after chemotherapy.

  Journal of biomedical optics 20100101

• Phase I and biomarker study of ABT-869, a multiple receptor tyrosine kinase inhibitor, in patients with refractory solid malignancies.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20091001

• Effect of the multitargeted receptor tyrosine kinase inhibitor, ABT-869 [N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea], on blood pressure in conscious rats and mice: reversal with antihypertensive agents and effect on tumor growth inhibition.

  The Journal of pharmacology and experimental therapeutics 20090601

• Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML.

  Blood 20090423

• ETA receptor blockade with atrasentan prevents hypertension with the multitargeted tyrosine kinase inhibitor ABT-869 in telemetry-instrumented rats.

  Journal of cardiovascular pharmacology 20090201

• ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside.

  Journal of hematology & oncology 20090101

• Simultaneous determination of a hydrophobic drug candidate and its metabolite in human plasma with salting-out assisted liquid/liquid extraction using a mass spectrometry friendly salt.

  Journal of pharmaceutical and biomedical analysis 20081201

• ABT-869, a multi-targeted tyrosine kinase inhibitor, in combination with rapamycin is effective for subcutaneous hepatocellular carcinoma xenograft.

  Journal of hepatology 20081201

• 7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

  Journal of medicinal chemistry 20080710

• In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptor.

  Leukemia research 20080701

• 3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.

  Journal of medicinal chemistry 20080313

• Synergistic antileukemic effects between ABT-869 and chemotherapy involve downregulation of cell cycle-regulated genes and c-Mos-mediated MAPK pathway.

  Leukemia 20080101

• Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.

  Bioorganic & medicinal chemistry letters 20080101

• A quantitative analysis of kinase inhibitor selectivity.

  Nature biotechnology 20080101

• ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia.

  Blood 20070415

• Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

  Journal of medicinal chemistry 20070405

• Hypoxia-inducible factor-1 inhibition in combination with temozolomide treatment exhibits robust antitumor efficacy in vivo.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20060801

• Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.

  Molecular cancer therapeutics 20060401

• Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors.

  Molecular cancer therapeutics 20060401

• A high-throughput, fully automated liquid/liquid extraction liquid chromatography/mass spectrometry method for the quantitation of a new investigational drug ABT-869 and its metabolite A-849529 in human plasma samples.

  Rapid communications in mass spectrometry : RCM 20060101

• A high-throughput liquid chromatography/tandem mass spectrometry method for simultaneous quantification of a hydrophobic drug candidate and its hydrophilic metabolite in human urine with a fully automated liquid/liquid extraction.

  Rapid communications in mass spectrometry : RCM 20060101