A multi-targeted receptor tyrosine kinase inhibitor
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Pexidartinib

Item No. 18271

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine
CAS Number
1029044-16-3
Synonyms
  • ​PLX3397
Molecular Formula
C20H15ClF3N5
Formula Weight
417.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 20 mg/ml
λmax
235, 303 nm
SMILES
ClC1=CC2=C(N=C1)NC=C2CC3=CN=C(NCC4=CN=C(C(F)(F)F)C=C4)C=C3
InChi Code
InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29)
InChi Key
JGWRKYUXBBNENE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $127

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    25 mg

    $297

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    50 mg

    $461

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    Product Description

    Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).1 It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.1 Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. DeNardo, D.G., Brennan, D.J., Rexhepaj, E., et al. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 1(1), 54-67 (2011).

    2. Coniglio, S.H., Eugenin, E., Dobrenis, K., et al. Microglial stimulation of glioblastoma invasion involves epidermal growth factor receptor (EGFR) and colony stimulating factor 1 receptor (CSF-1R) signaling. Mol. Med. 18(1), 519-527 (2012).