Pexidartinib (PLX3397)
new
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206178

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.


Price and Availability

Size
Price

50mg
USD 120
500mg
USD 785
5g
USD 3950
Size
Price

100mg
USD 190
1g
USD 1450
10g
USD 5950
Size
Price

200mg
USD 350
2g
USD 2450

Pexidartinib, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 50g may be 2 weeks.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 206178
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


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

InChi Key: JGWRKYUXBBNENE-UHFFFAOYSA-N

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)

SMILES Code: FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F


Technical Data

Appearance:
Yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (MSDS):

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).

Solubility:
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).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Shiao SL, Ruffell B, DeNardo D, Faddegon B, Park CC, Coussens LM. TH2-polarized CD4+ T cells and macrophages limit efficacy of radiation therapy. Cancer Immunol Res. 2015 Feb 25. pii: canimm.0232.2014. [Epub ahead of print] PubMed PMID: 25716473.

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.

3: De I, Nikodemova M, Steffen MD, Sokn E, Maklakova VI, Watters JJ, Collier LS. CSF1 overexpression has pleiotropic effects on microglia in vivo. Glia. 2014 Dec;62(12):1955-67. doi: 10.1002/glia.22717. Epub 2014 Jul 5. PubMed PMID: 25042473; PubMed Central PMCID: PMC4205273.

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.

5: Kim TS, Cavnar MJ, Cohen NA, Sorenson EC, Greer JB, Seifert AM, Crawley MH, Green BL, Popow R, Pillarsetty N, Veach DR, Ku AT, Rossi F, Besmer P, Antonescu CR, Zeng S, Dematteo RP. Increased KIT inhibition enhances therapeutic efficacy in gastrointestinal stromal tumor. Clin Cancer Res. 2014 May 1;20(9):2350-62. doi: 10.1158/1078-0432.CCR-13-3033. Epub 2014 Feb 28. PubMed PMID: 24583793; PubMed Central PMCID: PMC4008656.

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.