XL01126

Tocris Bioscience | Catalog # 8968

Potent and selective LRRK2 Degrader (PROTAC®)
Tocris Bioscience
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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 Dundee

Product Specifications for XL01126

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.

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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.

Select a batch to recalculate based on the batch molecular weight:

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

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Background References

References are publications that support the biological activity of the product.

Product Documents for XL01126

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for XL01126

For research use only

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