Biological Activity
Potent TBK1 (TANK-binding kinase-1) inhibitor (IC50 = 6 nM). Inhibits the formation of autophagosomes in lung cancer cells.
Technical Data
| M. Wt | 487.04 |
| Formula | C25H34N6O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 121513855 |
| InChI Key | BOBHGYDEKISHIZ-UHFFFAOYSA-N |
| Smiles | O=C(C1CCC1)NCCCNC2=C(C3CC3)C=NC(NC4=CC=C(N5CCOCC5)C=C4)=N2.Cl |
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 | |||
| DMSO | 48.7 | 100 | |
| ethanol | 48.7 | 100 | |
| water | 48.7 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 487.04. 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 | 2.05 mL | 10.27 mL | 20.53 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.11 mL |
| 10 mM | 0.21 mL | 1.03 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Newman et al (2012) TBK1 kinase addiction in lung cancer cells is mediated via autophagy of Tax1bp1/Ndp52 and non-canonical NF-κB signalling. PLoS ONE 7 e50672 PMID: 23209807
McIver et al (2012) Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases. Bioorg.Med.Chem.Lett. 22 7169 PMID: 23099093
Keywords: MRT 68601 hydrochloride, supplier, MRT68601, hydrochloride, potent, TBK1, TANK-binding, kinase-1, inhibitors, inhibits, autophagy, autophagosomes, Other, Kinases, Autophagy, Other, Kinases, Tocris Bioscience
