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CAS#: 1029044-16-3

Description: Pexidartinib, also know as PLX-3397, is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor PLX3397 binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease.

Synonym: PLX3397; PLX-3397; PLX 3397; Pexidartinib

IUPAC/Chemical Name: 5-((5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine


Name: Pexidartinib (PLX3397)
CAS#: 1029044-16-3
Chemical Formula: C20H15ClF3N5
Exact Mass: 417.09681
Molecular Weight: 417.81
Elemental Analysis: C, 57.49; H, 3.62; Cl, 8.49; F, 13.64; N, 16.76


Yellow solid powder
>98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition:
Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 – 4 C for short term (days to weeks), or -20 C for long term (months).


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2: Sluijter M, van der Sluis TC, van der Velden PA, Versluis M, West BL, van der Burg SH, van Hall T. Inhibition of CSF-1R supports T-cell mediated melanoma therapy. PLoS One. 2014 Aug 11;9(8):e104230. doi: 10.1371/journal.pone.0104230. eCollection 2014. PubMed PMID: 25110953; PubMed Central PMCID: PMC4128661.

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4: Patwardhan PP, Surriga O, Beckman MJ, de Stanchina E, Dematteo RP, Tap WD, Schwartz GK. Sustained inhibition of receptor tyrosine kinases and macrophage depletion by PLX3397 and rapamycin as a potential new approach for the treatment of MPNSTs. Clin Cancer Res. 2014 Jun 15;20(12):3146-58. doi: 10.1158/1078-0432.CCR-13-2576. Epub 2014 Apr 9. PubMed PMID: 24718867; PubMed Central PMCID: PMC4060793.

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6: Slade Shantz JA, Yu YY, Andres W, Miclau T 3rd, Marcucio R. Modulation of macrophage activity during fracture repair has differential effects in young adult and elderly mice. J Orthop Trauma. 2014;28 Suppl 1:S10-4. doi: 10.1097/BOT.0000000000000062. PubMed PMID: 24378434; PubMed Central PMCID: PMC3965608.

7: Mok S, Koya RC, Tsui C, Xu J, Robert L, Wu L, Graeber TG, West BL, Bollag G, Ribas A. Inhibition of CSF-1 receptor improves the antitumor efficacy of adoptive cell transfer immunotherapy. Cancer Res. 2014 Jan 1;74(1):153-61. doi: 10.1158/0008-5472.CAN-13-1816. Epub 2013 Nov 18. PubMed PMID: 24247719; PubMed Central PMCID: PMC3947337.

8: Abou-Khalil R, Yang F, Mortreux M, Lieu S, Yu YY, Wurmser M, Pereira C, Relaix F, Miclau T, Marcucio RS, Colnot C. Delayed bone regeneration is linked to chronic inflammation in murine muscular dystrophy. J Bone Miner Res. 2014 Feb;29(2):304-15. doi: 10.1002/jbmr.2038. PubMed PMID: 23857747; PubMed Central PMCID: PMC3893315.

9: Hatzimichael E, Georgiou G, Benetatos L, Briasoulis E. Gene mutations and molecularly targeted therapies in acute myeloid leukemia. Am J Blood Res. 2013;3(1):29-51. Epub 2013 Jan 17. PubMed PMID: 23358589; PubMed Central PMCID: PMC3555190.

10: He Y, Rhodes SD, Chen S, Wu X, Yuan J, Yang X, Jiang L, Li X, Takahashi N, Xu M, Mohammad KS, Guise TA, Yang FC. c-Fms signaling mediates neurofibromatosis Type-1 osteoclast gain-in-functions. PLoS One. 2012;7(11):e46900. doi: 10.1371/journal.pone.0046900. Epub 2012 Nov 7. PubMed PMID: 23144792; PubMed Central PMCID: PMC3492362.

11: Prada CE, Jousma E, Rizvi TA, Wu J, Dunn RS, Mayes DA, Cancelas JA, Dombi E, Kim MO, West BL, Bollag G, Ratner N. Neurofibroma-associated macrophages play roles in tumor growth and response to pharmacological inhibition. Acta Neuropathol. 2013 Jan;125(1):159-68. doi: 10.1007/s00401-012-1056-7. Epub 2012 Oct 26. PubMed PMID: 23099891; PubMed Central PMCID: PMC3547628.

12: Chitu V, Nacu V, Charles JF, Henne WM, McMahon HT, Nandi S, Ketchum H, Harris R, Nakamura MC, Stanley ER. PSTPIP2 deficiency in mice causes osteopenia and increased differentiation of multipotent myeloid precursors into osteoclasts. Blood. 2012 Oct 11;120(15):3126-35. doi: 10.1182/blood-2012-04-425595. Epub 2012 Aug 24. PubMed PMID: 22923495; PubMed Central PMCID: PMC3471520.

13: Coniglio SJ, Eugenin E, Dobrenis K, Stanley ER, West BL, Symons MH, Segall JE. Microglial stimulation of glioblastoma invasion involves epidermal growth factor receptor (EGFR) and colony stimulating factor 1 receptor (CSF-1R) signaling. Mol Med. 2012 May 9;18:519-27. doi: 10.2119/molmed.2011.00217. PubMed PMID: 22294205; PubMed Central PMCID: PMC3356419.

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