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Tocris/GSK 1838705/5111/10/10 mg

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货号: 5111/10

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

GSK 1838705 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 532.57. Batch specific molecular weights may vary from batch to batch due to solvent 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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Sabbatini et al (2009) 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. 8 2811 PMID: 19825801

Gao et al (2014) Site-specific activation of AKT protects cells from death induced by glucose deprivation. Oncogene 33 745 PMID: 23396361

Chamberlain et al (2009) Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg.Med.Chem.Lett. 19 360 PMID: 19071018

Keywords: GSK 1838705, supplier, GSK1838705, potent, and, selective, IR, and, IGF1R, inhibitors, inhibits, antitumor, insulin, receptor, like, growth, factor, 1, anaplastic, lymphoma, kinase, ALK, Insulin, and, Insulin-like, Receptors, Insulin, and, insulin-like, Receptors, ALK, Insulin, and, insulin-like, Receptors, Tocris Bioscience

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