Lestaurtinib | Tocris Bioscience 3395 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

Lestaurtinib

catalog :

3395

quantity :

1 mg

price :

266 USD

more info or order :

Tocris Bioscience product webpage

citations: 7

Reference
Pinto N, Prokopec S, Vizeacoumar F, Searle K, Lowerison M, Ruicci K, et al. Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models. PLoS ONE. 2018;13:e0207152 pubmed publisher
Beck D, Zobel J, Barber R, Evans S, Lezina L, Allchin R, et al. Synthetic Lethal Screen Demonstrates That a JAK2 Inhibitor Suppresses a BCL6-dependent IL10RA/JAK2/STAT3 Pathway in High Grade B-cell Lymphoma. J Biol Chem. 2016;291:16686-98 pubmed publisher
Rogers S, Gahring L. Upregulation of Nicotinic Acetylcholine Receptor alph4+beta2 through a Ligand-Independent PI3Kbeta Mechanism That Is Enhanced by TNFalpha and the Jak2/p38Mapk Pathways. PLoS ONE. 2015;10:e0143319 pubmed publisher
Gaji R, Checkley L, Reese M, Ferdig M, Arrizabalaga G. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014;58:2598-607 pubmed publisher
Gäbler K, Rolvering C, Kaczor J, Eulenfeld R, Méndez S, Berchem G, et al. Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J Cell Mol Med. 2013;17:265-76 pubmed publisher
Deshpande A, Reddy M, Schade G, Ray A, Chowdary T, Griffin J, et al. Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia. 2012;26:708-15 pubmed publisher
Kharazi S, Mead A, Mansour A, Hultquist A, Böiers C, Luc S, et al. Impact of gene dosage, loss of wild-type allele, and FLT3 ligand on Flt3-ITD-induced myeloproliferation. Blood. 2011;118:3613-21 pubmed publisher

product information

brand :

Tocris

master code :

3395

SKU :

3395/1

product name :

Lestaurtinib

description :

JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB

target :

JAK Kinase Inhibitors

category :

Small Molecules

unit size :

1 mg

purity :

99%

observed molecular weight :

439.46

url print :

?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

Potent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and 25 nM, respectively). Also inhibits Aurora kinase A and B (IC50 values are 8.1 and 2.3 nM, respectively) and prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo .

catalog number base :

3395

product keywords :

TrkA JAK2 FLT3 inhibitors inhibits Neurotrophin Receptors Tyrosine Kinases RTKs Janus-Activated CEP701 aurora kinases AurA AurB CEP-701 JAK Kinase Trk Receptors FLT3 Aurora Kinases 3395,

extended description :

JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB

chemical name text :

(9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3 ,2 ,1 -kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one

formula :

C 26 H 21 N 3 O 4

formula text :

C26H21N3O4

cas num :

111358-88-4

2020 USD :

255

2021 USD :

266 USD

alt names :

CEP-701

storage :

Desiccate at -20°C

more info or order :

Tocris Bioscience product webpage