A brain-penetrant CSF1R inhibitor (IC50 = 0.016 µM); selective for CSF1R over FLT3

PLX5622 – 25 mg

Brand:
Cayman
CAS:
1303420-67-8
Storage:
-20
UN-No:
- /

PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).{53727} It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and kinase insert domain receptor (KDR; IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively) and is greater than 100-fold selective for CSF1R over a panel of 230 kinases.{53727,53728} PLX5622 (65 mg/kg) reduces the number of Iba-1+ cells, a marker of reduced microglia activation, in the dorsal horn of the spinal cord in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve.{53728} It also decreases macrophage levels of TNF-α and IL-1β and infiltration into the sciatic nerve, as well as alleviates mechanical and cold allodynia in the same model. Dietary administration of PLX5622 (1,200 ppm in chow) decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical amyloid-β (Aβ) plaques in the 5XFAD transgenic mouse model of Alzheimer’s disease.{53727}  

 

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Description

A brain-penetrant CSF1R inhibitor (IC50 = 0.016 µM); selective for CSF1R over FLT3, Kit, Aurora C, and KDR (IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively); greater than 100-fold selective for CSF1R over a panel of 230 kinases; reduces the number of Iba-1+ cells in the spinal cord dorsal horn in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve at 65 mg/kg; decreases macrophage levels of TNF-α and IL-1β and infiltration in the sciatic nerve and alleviates mechanical and cold allodynia in the same model; decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical Aβ plaques in the 5XFAD mouse model of Alzheimer’s disease at 1,200 ppm

Formal name: 5-fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy-3-pyridinemethanamine

Synonyms: 

Molecular weight: 395.4

CAS: 1303420-67-8

Purity: ≥98%

Formulation: A crystalline solid

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