GSK 1838705

Name: GSK 1838705
Brand: Tocris Bioscience
SKU: 5111

Tocris Bioscience a Bio-Techne Brand

Catalog # 5111

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Key Product Details

Description:	Potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK)
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
Purity:	≥98% (HPLC)
Molecular Weight:	532.57

View Full Technical Details for GSK 1838705

Biological Activity for GSK 1838705

GSK 1838705 is a potent insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) inhibitor (IC₅₀ values are 1.6 and 2 nM, respectively). Also inhibits anaplastic lymphoma kinase (ALK) (IC₅₀ = 0.5 nM). Displays > 800-fold selectivity for IR, IGFR1 and ALK over a panel of 44 kinases including JNK. Blocks proliferation of cancer cell lines in vitro, and causes complete regression of ALK-dependent tumors in vivo. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Compound Libraries for GSK 1838705

GSK 1838705 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK 1838705

M. Wt	532.57
Formula	C₂₇H₂₉FN₈O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1116235-97-2
PubChem ID	25182616
InChi Key	HZTYDQRUAWIZRE-UHFFFAOYSA-N
Smiles	O=C(CN(C)C)N4CCC(C4=C5)=CC(OC)=C5NC1=NC(NC3=C(C(NC)=O)C(F)=CC=C3)=C2C(NC=C2)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 1838705

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	53.26	100

Preparing Stock Solutions for GSK 1838705

The following data is based on the product molecular weight 532.57.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.88 mL	9.39 mL	18.78 mL
5 mM	0.38 mL	1.88 mL	3.76 mL
10 mM	0.19 mL	0.94 mL	1.88 mL
50 mM	0.04 mL	0.19 mL	0.38 mL

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References for GSK 1838705

References are publications that support the biological activity of the product.

Gao Site-specific activation of AKT protects cells from death induced by glucose deprivation. Oncogene 2014 PMID: 23396361
Sabbatini GSK1838705A inhibits the Ins-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol.Cancer.Ther. 2009 PMID: 19825801
Chamberlain Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg.Med.Chem.Lett. 2009 PMID: 19071018

Citations for GSK 1838705

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