Biological Activity
Potent and selective LRRK2 inhibitor (IC50 values are 2.2, 6.6 and 47.7 nM for G2019S-mutant, wild-type and A2016T-mutant LRRK2, respectively). Selective for LRRK2 over a panel of 138 kinases. Brain penetrant and orally bioavailable.
Licensing Information
Sold under license from Dana-Farber Cancer Institute.
Technical Data
| M. Wt | 416.87 |
| Formula | C19H21ClN6O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1700693-08-8 |
| Smiles | O=C(N1CCOCC1)C2=CC(OC)=C(NC3=NC(NC)=C(C(Cl)=CN4)C4=N3)C=C2 |
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 | 41.69 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 416.87. 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 | 2.4 mL | 11.99 mL | 23.99 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.8 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.4 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hatcher et al (2015) Discovery of a pyrrolopyrimidine (JH-II-127), a highly potent, selective, and brain penetrant LRRK2 inhibitor. ACS Med.Chem.Lett. 6 584 PMID: 26005538
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