| CAS NO: | 1191911-27-9 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1191911-27-9 |
| 化学名 | (E)-N-(2-((5-chloro-2-((2-methoxy-4-morpholinophenyl)amino)pyrimidin-4(3H)-ylidene)amino)phenyl)methanesulfonamide hydrochloride |
| Canonical SMILES | COC1=C(NC2=NC=C(Cl)/C(N2)=N\C3=CC=CC=C3NS(C)(=O)=O)C=CC(N4CCOCC4)=C1.Cl |
| 分子式 | C22H25ClN6O4S.HCl |
| 分子量 | 541.45 |
| 溶解度 | DMF: 20 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 10 mg/mL |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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%. References: |
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