CZC-54252
Modify Date: 2024-01-10 21:49:01
CZC-54252 structure
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Common Name | CZC-54252 | ||
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| CAS Number | 1191911-27-9 | Molecular Weight | 504.990 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 718.1±70.0 °C at 760 mmHg | |
| Molecular Formula | C22H25ClN6O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 388.1±35.7 °C | |
Use of CZC-54252CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.IC50 value: 1.28 nM/1.85 nM(LRRK2/G2019S LRRK2) [1]Target: LRRK2 inhibitorin vitro: 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 [1]. G2019S LRRK2-induced human neuronal injury was attenuated by CZC-25146 with an EC50 of ~4 nM (EC50 CZC-54252 ~1 nM) and fully reversed to wild-type levels by both compounds at concentrations as low as 8 nM (1.6 nM for CZC-54252) [2].in vivo: In vivo pharmacology established a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/h/kg for CZC-25146 (19). Unfortunately, it exhibited a poor brain penetration of just 4%. |
| Name | N-(2-(5-chloro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide |
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| Synonym | More Synonyms |
| Description | CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.IC50 value: 1.28 nM/1.85 nM(LRRK2/G2019S LRRK2) [1]Target: LRRK2 inhibitorin vitro: 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 [1]. G2019S LRRK2-induced human neuronal injury was attenuated by CZC-25146 with an EC50 of ~4 nM (EC50 CZC-54252 ~1 nM) and fully reversed to wild-type levels by both compounds at concentrations as low as 8 nM (1.6 nM for CZC-54252) [2].in vivo: In vivo pharmacology established a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/h/kg for CZC-25146 (19). Unfortunately, it exhibited a poor brain penetration of just 4%. |
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| Related Catalog | |
| References |
| Density | 1.5±0.1 g/cm3 |
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| Boiling Point | 718.1±70.0 °C at 760 mmHg |
| Molecular Formula | C22H25ClN6O4S |
| Molecular Weight | 504.990 |
| Flash Point | 388.1±35.7 °C |
| Exact Mass | 504.134644 |
| PSA | 126.09000 |
| LogP | 1.67 |
| Appearance of Characters | white solid |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.667 |
| Storage condition | -20℃ |
| Methanesulfonamide, N-[2-[[5-chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- |
| czc 54252 hydrochloride |
| N-{2-[(5-Chloro-2-{[2-methoxy-4-(4-morpholinyl)phenyl]amino}-4-pyrimidinyl)amino]phenyl}methanesulfonamide |
| CZC-54252 |