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Pexidartinib

Time:2016-11-01

Pexidartinib__PLX3397_

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

THEORETICAL ANALYSIS

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

TECHNICAL DATA

Appearance:
Yellow solid powder
Purity:
>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).
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).

REFERENCES

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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.

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