GSK1838705A

Hersteller MedChem Express
Kategorie Produkte / Inhibitors
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mM*1mL (in DMSO)
ArtNr HY-13020-10mM
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
GSK 1838705A, GSK-1838705A
CAS No.
1116235-97-2
Purity
>98%
MW
5325693
Formula
C27H29FN8O3
Solubility
10 mM in DMSO
Biological Description
GSK1838705A is a potent small-molecule IGF-1R, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively.
IC50 value: 2.0/1.6/0.5 nM ( IGF-1R/InsR/ALK)
Target: IGF-1R/InsR/ALK
GSK1838705A prevents the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing’s sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were obtained at efficacious doses. A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg led to 35% and 65% prevention of IGF-IR phosphorylation, respectively, whereas doses >=1 mg/kg led to complete inhibition of ligand-induced IGF-IR phosphorylation. Meanwhile, at a dose of 30 mg/kg, prevention was lasted for 24 hours after compound injection. GSK1838705A also suppresses the anaplastic lymphoma kinase (ALK), which mediates the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non–small cell lung cancers. Due to its inhibition of ALK, GSK1838705A gives rise to complete regression of ALK-dependent tumors in vivo at well-tolerated doses.
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 10mM*1mL (in DMSO)
Lieferbar: In stock
Listenpreis: 255,71 €
Preis: 255,71 €
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