GSK1838705A Inhibitor CAS No. 1116235-97-2

Cat. No.	Name	Size	Price
KI0552	GSK1838705A	5 mg	$272
	GSK1838705A	10 mg	$512
	GSK1838705A	50 mg	$1552
	GSK1838705A	200 mg	$3952

Chemical Characteristic

Product Name	GSK1838705A
CAS No.	1116235-97-2
Molecular Weight	532.57
Formula	C₂₇H₂₉FN₈O₃
Chemical Name	2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide
Smiles	C(=O)(c1c(cccc1F)Nc1c2c(nc(n1)Nc1c(cc3CCN(c3c1)C(=O)CN(C)C)OC)[nH]cc2)NC
Chemical Structure

Biological activities

GSK1838705A is a small-molecule IGF-IR and the insulin receptor inhibitor. The IC50 of GSK1838705A is 2 and 1.6 nM against IGF-IR and insulin receptor, respectively. GSK1838705A blocks the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing's sarcoma. GSK1838705A inhibits JNK1, JNK2 and JNK3 with IC50 of 5, 8 and 2 nM, respectively. GSK1838705A inhibits ligand-induced phosphorylation of IGF-IR and IR in a concentration-dependent manner, with a parallel decrease in phosphorylated AKT, IRS-1, and ERK. Flow cytometric analysis of MCF-7 and NCI-H929 cells treated with GSK1838705A reveals an accumulation of cells predominantly in G1(2N) phase of the cell cycle. GSK1838705A also inhibits the anaplastic lymphoma kinase (ALK) with an IC50 of 0.5 nM. GSK1838705A causes complete regression of ALK-dependent tumors in vivo at well-tolerated doses. A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg inhibits IGF-IR phosphorylation by 35% and 65% respectively, whereas doses ?? mg/kg results in complete inhibition of ligand-induced IGF-IR phosphorylation. GSK1838705A retards the growth of human tumor xenografts in vivo. In HT29 xenograft??earing mice, 60 mg/kg GSK1838705A causes a 42% tumor growth inhibition relative to vehicle-treated controls at the end of the treatment period, with no significant changes in body weight. ^[1]

Protocols

GSK1838705A is dissolved in DMSO at 10 mM.^[1]

References

[1] Sabbatini P, 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(10): 2811-2820.

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