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Lestaurtinib - ≥98%, high purity , Tyrosine-protein kinase receptor RET inhibitor, CAS No.111358-88-4, Tyrosine-protein kinase receptor RET inhibitor

  • Moligand™
  • ≥98%
Item Number
L275009
Grouped product items
SKUSizeAvailabilityPrice Qty
L275009-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$177.90
L275009-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$690.90

Potent JAK2, FLT3 and TrkA receptor tyrosine kinase inhibitor

Basic Description

SynonymsLestaurtinib|111358-88-4|CEP-701|KT-5555|SPM-924|KT5555|CEP 701|SP924|SP 924|SP-924|KT 5555|KT-555|CEP701|CHEMBL603469|DO989GC5D1|DTXSID5046778|A-154475.0|NCGC00168772-01|(5S,6S,8R)-6-hydroxy-6-(hydroxymethyl)-5-methyl-7,8,14,15-tetrahydro-5H-16-oxa-4b,8a
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent JAK2, FLT3 and TrkA receptor tyrosine kinase inhibitor (IC 50 values are 0.9, 3 and 25 nM respectively). Antiproliferative effects in vitro . Antileukemic agent in vivo . Orally active.
Storage TempProtected from light,Store at -20°C,Desiccated
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionTyrosine-protein kinase receptor RET inhibitor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.

Product Properties

ALogP2.2

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FAM120AOS Tdark Uncharacterized protein FAM120AOS 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DNAJA1 Tchem DnaJ homolog subfamily A member 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDKL5 Tchem Cyclin-dependent kinase-like 5 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK18 Tchem Cyclin-dependent kinase 18 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 21 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR2 Tclin Fibroblast growth factor receptor 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PLK4 Tchem Serine/threonine-protein kinase PLK4 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM3 Tchem Serine/threonine-protein kinase pim-3 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKG2 Tchem cGMP-dependent protein kinase 2 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKCH Tchem Protein kinase C eta type 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKD1 Tchem Serine/threonine-protein kinase D1 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ATR Tchem Serine/threonine-protein kinase ATR 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKB Tchem Aurora kinase B 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AAK1 Tchem AP2-associated protein kinase 1 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name (15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one
INCHI InChI=1S/C26H21N3O4/c1-25-26(32,12-30)10-18(33-25)28-16-8-4-2-6-13(16)20-21-15(11-27-24(21)31)19-14-7-3-5-9-17(14)29(25)23(19)22(20)28/h2-9,18,30,32H,10-12H2,1H3,(H,27,31)/t18-,25+,26+/m1/s1
InChi Key UIARLYUEJFELEN-LROUJFHJSA-N
Canonical SMILES CC12C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)(CO)O
Isomeric SMILES C[C@@]12[C@](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)(CO)O
PubChem CID 126565
Molecular Weight 439.46

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Chemical and Physical Properties

SolubilitySoluble in DMSO to 10 mM
SensitivityLight sensitive

Related Documents

References

1. Levis M, Allebach J, Tse KF, Zheng R, Baldwin BR, Smith BD, Jones-Bolin S, Ruggeri B, Dionne C, Small D.  (2002)  A FLT3-targeted tyrosine kinase inhibitor is cytotoxic to leukemia cells in vitro and in vivo..  Blood,  99  (11): (3885-91).  [PMID:12010785]
2. Vazquez-Ortiz G, Chisholm C, Xu X, Lahusen TJ, Li C, Sakamuru S, Huang R, Thomas CJ, Xia M, Deng C.  (2014)  Drug repurposing screen identifies lestaurtinib amplifies the ability of the poly (ADP-ribose) polymerase 1 inhibitor AG14361 to kill breast cancer associated gene-1 mutant and wild type breast cancer cells..  Breast Cancer Res,  16  (3): (R67).  [PMID:24962108]
3. Lee M & Rhee I.  (2017)  Cytokine Signaling in Tumor Progression..  Immune Netw,  17  (4): (214-227).  [PMID:28860951]
4. Chang J et al..  (2018)  Exome-wide analysis identifies three low-frequency missense variants associated with pancreatic cancer risk in Chinese populations..  Nat Commun,  (3688).  [PMID:30206226]

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