| Identification | Back Directory | [Name]
PLX5622 | [CAS]
1303420-67-8 | [Synonyms]
PLX5622
PLX 5622;PLX-5622
PLX5622 USP/EP/BP
5-Fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy-3-pyridinemethanamine
3-Pyridinemethanamine, 5-fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy- | [Molecular Formula]
C21H19F2N5O | [MDL Number]
MFCD32201039 | [MOL File]
1303420-67-8.mol | [Molecular Weight]
395.41 |
| Chemical Properties | Back Directory | [density ]
1.364±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (>25 mg/ml) | [form ]
solid | [pka]
13?+-.0.40(Predicted) | [color ]
Pale yellow | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
PLX5622 (1303420-67-8) is a highly selective (>20 fold over KIT and FLT3, >60 fold over 200 other kinases) and brain-penetrant inhibitor of colony-stimulating factor 1 receptor (CSF1R; IC50 = 16 nM).1 It prevented plaque formation in 5xFAD1 and 3xTg2 mouse models of Alzheimer’s disease via elimination of microglia in a CSF1R-dependent manner.? PLX5622 showed efficacy in a mouse neuropathic pain model via reduction of CD86+ macrophages resulting in reduced expression of pro-inflammatory cytokines.3 It also was able to ameliorate peripheral neuropathy in aging mice.4 PLX5622 displayed neuroprotective effects during the chronic phase of a traumatic brain injury mouse model.5? PLX5622 has also been shown to affect myeloid and lymphoid compartments, indicating that its affects are not limited to microglia and include peripheral immune cells.6 | [storage]
Store at -20°C | [References]
Spangenberg et al. (2019) Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer’s disease model; Nat. Commun.?10 3758
Dagher et al. (2015) Colony-stimulating factor 1 receptor inhibition prevents microglial plaque association and improves cognition in 3xTg-AD mice; J.? Neuroinflammation 12 139
Lee et al. (2018) Targeting macrophage and microglia activation with colony stimulating factor 1 receptor inhibitor is an effective strategy to treat injury-triggered neuropathic pain; Mol.? Pain?14 1
Yaun et al. (2018) Macrophage Depletion Ameliorates Peripheral Neuropathy in Aging Mice.; J.? Neurosci.?38 4610
Henry et al. (2020) Microglial Depletion with CSF1R Inhibitor During Chronic Phase of Experimental Traumatic Brain Injury Reduces Neurodegeneration and Neurological Deficits.; J.? Neurosci.?40 2960
Lei et al. (2020) CSF1R inhibition by a small-molecule inhibitor is not microglia specific; affecting hematopoiesis and the function of macrophages.; Proc. ?Natl. Acad. Sci USA?117 23336 |
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