| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
CZC-54252 is a potent, selective, and metabolically stable LRRK2 inhibitor (Leucine-rich repeat kinase-2) with IC50 of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively. CZC-25146 prevents mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency. CZC-54252 inhibited the activity of recombinant human wild-type LRRK2 with an IC50 ranging from 1 to 5 nM. The G2019S mutant was inhibited with an IC50 ranging from ～2 to ～7 nM in a TF-FRET assay. In addition, they were screened against a kinase panel of 185 kinases and exhibited good selectivity. CZC-25146 (19) inhibited five other kinases, PLK4, GAK, TNK1, CAMKK2, and PIP4K2C, with high potency only, but none of them have been classified as predictors of genotoxicity or hematopoietic toxicity.
| ln Vitro |
The recombinant human wild-type LRRK2 is inhibited by CZC-54252, with an IC50 ranging from approximately 1 to approximately 5 nM. They also demonstrated good selectivity when tested against a kinome of 185 kinases [1]. At 1.6 nM, CZC-54252 fully restored human neuronal damage to wild-type levels after attenuating G2019S LRRK2-induced neuronal damage with an EC50 of less than 1 nM [1].
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| ln Vivo |
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| Animal Protocol |
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| References | |||
| Additional Infomation |
CZC-25146 is a member of the class of aminopyrimidines that is 2,6-diamino-5-chloropyrimidine in which the amino groups at positions 2 and 6 are respectively carrying 2-methoxy-4-(morpholin-4-yl)phenyl and 2-(methanesulfonylamino)phenyl substituents. It is an inhibitor of the Parkinson's disease kinase LRRK2. It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor. It is an aminopyrimidine, a member of morpholines, an aromatic ether, an organochlorine compound, a sulfonamide and a secondary amino compound.
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| Molecular Formula |
C22H25CLN6O4S
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|---|---|---|
| Molecular Weight |
504.99
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| Exact Mass |
504.134
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| CAS # |
1191911-27-9
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| Related CAS # |
CZC-54252 hydrochloride;1784253-05-9
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| PubChem CID |
44252734
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
718.1±70.0 °C at 760 mmHg
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| Flash Point |
388.1±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.667
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| LogP |
1.67
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
34
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| Complexity |
737
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CLGWUCNXOBLWFM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25ClN6O4S/c1-32-20-13-15(29-9-11-33-12-10-29)7-8-19(20)26-22-24-14-16(23)21(27-22)25-17-5-3-4-6-18(17)28-34(2,30)31/h3-8,13-14,28H,9-12H2,1-2H3,(H2,24,25,26,27)
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| Chemical Name |
N-[2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]phenyl]methanesulfonamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9802 mL | 9.9012 mL | 19.8024 mL | |
| 5 mM | 0.3960 mL | 1.9802 mL | 3.9605 mL | |
| 10 mM | 0.1980 mL | 0.9901 mL | 1.9802 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Chemoproteomics-based discovery of LRRK2 lead compounds.ACS Chem Biol.2011 Oct 21;6(10):1021-8. |
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CZC-25146 and CZC-54252 are potent and selective LRRK2 inhibitors.ACS Chem Biol.2011 Oct 21;6(10):1021-8. |
CZC-25146 and CZC-54252 potently attenuate mutant LRRK2-mediated toxicity in primary human neurons.ACS Chem Biol.2011 Oct 21;6(10):1021-8. |
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