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GSK1838705A | IGF-1R/IR/ALK inhibitor

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Price:
$169.00
Catalog #:
C4183-5
Quantity:


Product Description

GSK1838705A is a pyrrolopyrimidine-based inhibitor of IGF-1R, IR, and ALK with IC50s of 2.0, 1.6, and 0.5 nM, respectively. Despite its potency against the insulin receptor, no major effect on glucose homeostasis was observed at efficacious doses. [1] In NIH-3T3/USN and NIH-3T3-hIR cell lines GSK1838705A inhibits ligand-induced phosphorylation of IGF1R and IR in a concentration-dependent manner, with concomitant decrease in phosphorylated AKT, IRS-1, and ERK. Antiproflierative EC50s ranged from 20 nM to 8 uM, with most values
In IGF-1-induced mice xenografts, a single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg resulted in 35% and 65% inhibition sof IGF-1R phosphorylation; doses >1 mg/kg completely inhibited phosphorylation. [1]

In ALCL tumor cells bearing ALK fusion genes, proliferation was inhibited in a concentration-dependent manner with EC50s ranging from 24 to 88 nM. [1]


Technical information:

Chemical Formula:   C27H29FN8O3
CAS #:   1116235-97-2
Molecular Weight:   532.57
Purity:   > 98%
Appearance:   Off White
Chemical Name:   2-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-6-fluoro-N-methylbenzamide
Solubility:   Up to 100mM in DMSO
Synonyms:   GSK-1838705A, GSK 1838705A, GSK1838705A

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Sabbatini et al., GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol. Cancer. Ther. 2009, 8, 2811-2820. Pubmed ID: 19825801

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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