GSK 1838705
Tocris Bioscience, part of Bio-Techne | Catalog # 5111
Potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK)
Key Product Details
Description
Potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK)
Product Description
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.Product Specifications
Molecular Weight
532.57
Formula
C27H29FN8O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
- 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
- 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
Product Specific Notices for GSK 1838705
For research use only
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