General description
An orally bioavailable fluoro-diaminopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of LRRK2 activity (IC50 = 4.76 and 6.87 nM for hr-wt-LRRK2 and G2019S-LRRK2 mutant, respectively) with selectivity over PLK4, GAK, TNK1, CAMKK2, and PIP4K2C (IC50<300 nM) in a 185-kinase panel. Does neither exert cytotoxicity nor block neuronal development of human or rat cortical neurons at 1 µM. Shown to prevent GS-LRRK2-induced neuronal injury (EC50 ~4 nM) and G2019S- or R1441C-LRRK2-mediated neuronal death in both rat and human cortical neurons (EC50 ~ 100 nM). Even though exhibits favorable pharmacokinetic profile and metabolic stability, and yet suffers from limited blood brain barrier penetration (~4%).
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Ramsden, N., et al. 2011. ACS Chem. Biol.6, 1021.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 488.54 (free base basis). Empirical Formula: C22H25FN6O4S · xHCl. Quality Level: 100. Assay: ≥. 98% (HPLC). form: powder. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. color: gray to off-white. solubility: water: 1 . mg/mL, DMSO: 5 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: FC1: C(N: C(NC2: CC: C(N3CCOCC3)C: C2OC)N: C1)NC4: CC: CC: C4NS(: O)(C): O.[xHCl]. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51172444
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 438194-10MG
