PFE-360
- Product Name
- PFE-360
- CAS No.
- 1527475-61-1
- Chemical Name
- PFE-360
- Synonyms
- PFE-360;PF-06685360;PFE-360 ，E0998;PFE-360 (PF-06685360);PFE-360, 10 mM in DMSO;1-Methyl-4-(4-morpholino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-1H-pyrrole-2-carbonitrile;1H-Pyrrole-2-carbonitrile, 1-methyl-4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-;1-Methyl-4-(4-morpholino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-1H-pyrrole-2-carbonitrile , PFE-360;PF06685360,PF 06685360,LRRK2,inhibit,Inhibitor,PFE 360,PFE360,PFE-360,Leucine-rich repeat kinase 2
- CBNumber
- CB35419811
- Molecular Formula
- C16H16N6O
- Formula Weight
- 308.34
- MOL File
- 1527475-61-1.mol
PFE-360 Property
- storage temp.
- room temp
- solubility
- DMSO: 2 mg/mL, clear
- form
- powder
- color
- white to beige
PFE-360 Chemical Properties,Usage,Production
Description
PFE-360 (PF-06685360) is a poten and elective inhibitor of LRRK2 kinase.
Uses
PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo[1][2].
in vitro
PFE-360 (4 mg/kg and 7.5 mg/kg, orally, BID, 10-12 weeks) treatment potently decreases the LRRK2-pSer935/total LRRK2 ratio, with no significant adverse effects.
animal Model: Female Sprague Dawley rats (NTac:SD) weighed 225-250 g.
Dosage: 4 mg/kg and 7.5 mg/kg (pharmacokinetics and pharmacodynamics).
Administration: Orally BID for 10-12 weeks.
Result: The LRRK2-pSer935/total LRRK2 ratio was significantly decreased at both 1 h and 12 h after dosing.
The terminal bodyweights exhibited no significant changes.
in vivo
PFE-360 (4 mg/kg and 7.5 mg/kg, orally, BID, 10-12 weeks) treatment potently decreases the LRRK2-pSer935/total LRRK2 ratio, with no significant adverse effects[1].
| Animal Model: | Female Sprague Dawley rats (NTac:SD) weighed 225-250 g[3]. |
| Dosage: | 4 mg/kg and 7.5 mg/kg (pharmacokinetics and pharmacodynamics). |
| Administration: | Orally BID for 10-12 weeks. |
| Result: | The LRRK2-pSer935/total LRRK2 ratio was significantly decreased at both 1 h and 12 h after dosing. The terminal bodyweights exhibited no significant changes. |
References
[1] Marco A.S. Baptista, et al. LRRK2 Kinase Inhibitors of Different Structural Classes Induce Abnormal Accumulation of Lamellar Bodies in Type II Pneumocytes in Non-Human Primates but are Reversible and Without Pulmonary Functional Consequences.
[2] Andersen MA, et al. Parkinson's disease-like burst firing activity in subthalamic nucleus induced by AAV-α-synuclein is normalized by LRRK2 modulation. Neurobiol Dis. 2018 Aug;116:13-27. DOI:10.1016/j.nbd.2018.04.011
[3] Andersen MA, et al. PFE-360-induced LRRK2 inhibition induces reversible, non-adverse renal changes in rats. Toxicology. 2018 Feb 15;395:15-22. DOI:10.1016/j.tox.2018.01.003
PFE-360 Preparation Products And Raw materials
Raw materials
Preparation Products
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