GSK1838705A – 10 mg

Brand:
Cayman
CAS:
1116235-97-2
Storage:
-20
UN-No:
Non-Hazardous - /

GSK1838705A is an inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) and the insulin receptor (IR; IC50s = 2 and 1.6 nM, respectively).{41768} It is selective for IGF-1R and IR over a panel of 47 kinases (IC50s = >1,600 nM), however, it also inhibits anaplastic lymphoma kinase (ALK; IC50 = 0.5 nM). GSK1838705A inhibits IGF-1 and insulin-induced phosphorylation of IGF-1R and IR in a concentration-dependent manner as well as phosphorylation of the downstream signaling markers Akt, IRS-1, and ERK in MCF-7 breast carcinoma cells. It inhibits growth in a panel of cancer cell lines (EC50s = 24-8,378 nM) with the IGF-1R signaling-dependent multiple myeloma and Ewing’s sarcoma cell lines being the most sensitive. In vivo, GSK1838705A completely inhibits IGF-1-induced phosphorylation of IGF-1R, Akt, and IRS-1 as well as reduces tumor growth in the COLO 205 and NIH-3T2/LISN mouse xenograft models when administered at doses of ≥1 and ≥10 mg/kg, respectively. It also induces tumor cell apoptosis and reduces tumor growth in U87MG glioma and PC3R prostate cancer mouse xenograft models.{41769,41770}  

 

Available on backorder

SKU: 24904 - 10 mg Category:

Description

An IGF-1R and IR inhibitor (IC50s = 2 and 1.6 nM, respectively); selective for IGF-1R and IR over a panel of 47 kinases (IC50s = >1,600 nM); inhibits ALK (IC50 = 0.5 nM); inhibits ligand-induced phosphorylation of IGF-1R and IR as well as phosphorylation of Akt, IRS-1, and ERK in MCF-7 breast carcinoma cells; inhibits the growth of a panel of cancer cell lines (EC50s = 24-8,378 nM); completely inhibits IGF-1-induced phosphorylation of IGF-IR, Akt, and IRS-1 as well as reduces tumor growth in the COLO 205 and NIH-3T2/LISN mouse xenograft models at ≥1 and ≥10 mg/kg, respectively; induces tumor cell apoptosis and reduces tumor growth in U87MG glioma and PC3R prostate cancer mouse xenograft models


Formal name: 2-[[2-[[1-[2-(dimethylamino)acetyl]-2,3-dihydro-5-methoxy-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methyl-benzamide

Synonyms: 

Molecular weight: 532.6

CAS: 1116235-97-2

Purity: ≥95%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|IGF-1R/InsR Family||Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling