A CSF1R inhibitor
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Alternative(s)
28927PLX5622
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PLX5622 (hemifumarate)

Item No. 36277

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-fluoro-N-((5-fluoro-2-methoxypyridin-3-yl)methyl)-5-((5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2-amine, hemifumarate
Molecular Formula
C21H19F2N5O • 1/2C4H4O4
Formula Weight
485.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 16 mg/mlEthanol: Slightly solublePBS (pH 7.2): 0.3 mg/ml
λmax
218, 229, 292 nm
SMILES
CC1=CN=C(NC=C2CC3=CC=C(NCC4=C(OC)N=CC(F)=C4)N=C3F)C2=C1.OC(/C=C/C(O)=O)=O.CC5=CN=C(NC=C6CC7=CC=C(NCC8=C(OC)N=CC(F)=C8)N=C7F)C6=C5
InChi Code
InChI=1S/2C21H19F2N5O.C4H4O4/c2*1-12-5-17-14(9-26-20(17)25-8-12)6-13-3-4-18(28-19(13)23)24-10-15-7-16(22)11-27-21(15)29-2;5-3(6)1-2-4(7)8/h2*3-5,7-9,11H,6,10H2,1-2H3,(H,24,28)(H,25,26);1-2H,(H,5,6)(H,7,8)/b;;2-1+
InChi Key
FMEISBYRQFIJPD-WXXKFALUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $125

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    10 mg

    $203

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    25 mg

    $310

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    Product Description

    PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).1 It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and VEGFR2 (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.1,2 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.2 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.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Spangenberg, E., Severson, P.L., Hohsfield, L.A., et al. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer’s disease model. Nat. Commun. 10(1), 3758 (2019).

    2. Lee, S., Shi, X.Q., Fan, A., et al. 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, (2018).