XL01126 New
Tocris Bioscience, part of Bio-Techne | Catalog # 8968
Potent and selective LRRK2 Degrader (PROTAC®)
Key Product Details
Description
Potent and selective LRRK2 Degrader (PROTAC®)
Product Description
XL01126 is a potent LRRK2 Degrader (PROTAC®) effective in multiple cell lines (DC50 values within 15-72 nM, Dmax values range from 82-90%). Exhibits high cell permeability and forms a positively cooperative ternary complex with VHL and LRRK2, which compensates for a substantial loss of binary binding affinities to VHL and LRRK2, increasing its degradation performance in cells. Orally bioavailable (F=15%), XL01126 can penetrate the blood brain barrier after oral and parenteral dosing in mice.PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license
Licensing Information
Sold under licence from the University of DundeeProduct Specifications
Molecular Weight
1019.69
Formula
C50H64ClFN10O6S2
Storage
Store at -20°C
Purity
≥98%
Chemical Name
(2S,4R)-1-((R)-3-((((1r,4R)-4-((4-(4-((5-Chloro-4-(methyl-λ2-azaneyl)pyrimidin-2-yl)amino)-3-methoxybenzoyl)piperazin-1-yl)methyl)cyclohexyl)methyl)thio)-2-(1-fluorocyclopropane-1-carboxamido)-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS Number
3011029-58-3
PubChem ID
165412689
InChI Key
HKSBXNVKPFTBIG-SHFRUIRLSA-N
SMILES
O=C(C1(CC1)F)N[C@@H](C(C)(C)SC[C@H]2CC[C@@H](CC2)CN3CCN(CC3)C(C4=CC(OC)=C(C=C4)NC5=NC=C(Cl)C(NC)=N5)=O)C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C8=C(N=CS8)C)C=C7)=O)=O
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 | 101.97 | 100 |
Preparing Stock Solutions
for XL01126
The following data is based on the product molecular weight 1019.69
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 | 0.98 mL | 4.90 mL | 9.81 mL |
| 5 mM | 0.20 mL | 0.98 mL | 1.96 mL |
| 10 mM | 0.10 mL | 0.49 mL | 0.98 mL |
| 50 mM | 0.02 mL | 0.10 mL | 0.20 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
Product Specific Notices for XL01126
For research use only
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