936091-26-8 | Fedratinib (SAR302503, TG101348)

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$30.00	$21.00
5mg	95%	in stock	$54.00	$38.00
10mg	95%	in stock	$91.00	$64.00
25mg	95%	in stock	$163.00	$114.00
100mg	95%	in stock	$270.00	$189.00
250mg	95%	in stock	$529.00	$370.00
1g	95%	in stock	$1,390.00	$973.00

Description

• Catalog Number: AH85428
• Chemical Name: Fedratinib (SAR302503, TG101348)
• CAS Number: 936091-26-8
• Molecular Formula: C27H36N6O3S
• Molecular Weight: 524.6781
• MDL Number: MFCD12922515
• SMILES: Cc1cnc(nc1Nc1cccc(c1)S(=O)(=O)NC(C)(C)C)Nc1ccc(cc1)OCCN1CCCC1

Computed Properties

• Complexity: 787
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 37
• Hydrogen Bond Acceptor Count: 9
• Hydrogen Bond Donor Count: 3
• Rotatable Bond Count: 11
• XLogP3: 4.8

Literature

• Differences in gene expression and alterations in cell cycle of acute myeloid leukemia cell lines after treatment with JAK inhibitors.

  European journal of pharmacology 20151015

• Utilization of human nuclear receptors as an early counter screen for off-target activity: a case study with a compendium of 615 known drugs.

  Toxicological sciences : an official journal of the Society of Toxicology 20150601

• Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.

  Nature chemical biology 20140401

• Flavanoids induce expression of the suppressor of cytokine signalling 3 (SOCS3) gene and suppress IL-6-activated signal transducer and activator of transcription 3 (STAT3) activation in vascular endothelial cells.

  The Biochemical journal 20130901

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

  Bioorganic & medicinal chemistry letters 20130801

• Current outlook on molecular pathogenesis and treatment of myeloproliferative neoplasms.

  Molecular diagnosis & therapy 20121001

• JAK2 inhibitors and their impact in myeloproliferative neoplasms.

  Hematology (Amsterdam, Netherlands) 20120401

• New generation small-molecule inhibitors in myeloproliferative neoplasms.

  Current opinion in hematology 20120301

• Comprehensive analysis of kinase inhibitor selectivity.

  Nature biotechnology 20111030

• Targeting myeloproliferative neoplasms with JAK inhibitors.

  Current opinion in hematology 20110301

• JAK inhibitor therapy for myelofibrosis: critical assessment of value and limitations.

  Leukemia 20110201

• Octa-arginine mediated delivery of wild-type Lnk protein inhibits TPO-induced M-MOK megakaryoblastic leukemic cell growth by promoting apoptosis.

  PloS one 20110101

• Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.

  Bioorganic & medicinal chemistry letters 20101215

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

  Chemistry & biology 20101124

• Inhibition of JAK-STAT signaling by TG101348: a novel mechanism for inhibition of KITD816V-dependent growth in mast cell leukemia cells.

  Leukemia 20100701

• Physiological Jak2V617F expression causes a lethal myeloproliferative neoplasm with differential effects on hematopoietic stem and progenitor cells.

  Cancer cell 20100615

• Therapeutic potential of JAK2 inhibitors.

  Hematology. American Society of Hematology. Education Program 20090101

• TG101348, a JAK2-selective antagonist, inhibits primary hematopoietic cells derived from myeloproliferative disorder patients with JAK2V617F, MPLW515K or JAK2 exon 12 mutations as well as mutation negative patients.

  Leukemia 20080901

• Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.

  Cancer cell 20080401