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      Pexidartinib (PLX3397; Turalio; CML261; FP113)
      Pexidartinib (PLX3397; Turalio; CML261; FP113)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0630
      CAS #: 1029044-16-3Purity ≥98%

      Description: Pexidartinib (formerly PLX-3397; CML-261; FP-113; trade name Turalio) is an orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor of CSF-1R, Kit, and Flt3 with potential antineoplastic activity. It inhibits CSF-1R, Kit, and Flt3 with IC50s of 20 nM, 10 nM and 160 nM, respectively. In August 2019, Pexidartinib received FDA approval for treatment of giant-cell tumor of the tendon sheath (GC-TS). However, it is available in the US only through the Turalio Risk Evaluation and Mitigation Strategy (REMS) Program.

      References: Cancer Discov. 2011 Jun;1(1):54-67; Mol Med. 2012 May 9;18:519-27; Blood. 2012 Oct 11;120(15):3126-35.

      Related CAS: 2040295-03-0 (HCl); 1029044-16-3 (free base); 2169310-71-6 (2HCl)

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      Molecular Weight (MW)417.81
      FormulaC20H15ClF3N5
      CAS No.1029044-16-3 (free); 
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 83 mg/mL (198.6 mM)
      Water: <1 mg/mL
      Ethanol: <1 mg/mL
      Solubility (In vivo)10% DMSO+40% PEG 300+ddH2O: 15 mg/mL
      SynonymsPexidartinib; CML-261; FP-113; PLX3397; PLX 3397; CML 261; CML261; PLX-3397;FP 113; FP113; trade name Turalio

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

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


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      In Vitro

      In vitro activity: In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively.

      Kinase Assay: Pexidartinib (PLX-3397) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, shows 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC50s of 160, 350, 860, 880, and 890 nM, respectively. 

      In VivoIn MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma.
      Animal modelMMTV-PyMT mouse model
      Formulation & DosageFormulated in mouse chow;  40 mg/kg; p.o. administration
      ReferencesCancer Discov. 2011 Jun;1(1):54-67; Mol Med. 2012 May 9;18:519-27; Blood. 2012 Oct 11;120(15):3126-35.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      Pexidartinib (PLX3397)

      Combined PLX3397 and PTX treatment inhibits metastasis in a CD8-dependent manner. Cancer Discov. 2011 Jun 1; 1: 54–67.

      Pexidartinib (PLX3397)

      PTX in combination with PLX3397 induces antitumor T-cell response. Cancer Discov. 2011 Jun 1; 1: 54–67.

      Pexidartinib (PLX3397)

      CD68/CD4/CD8 immune signature is an independent prognostic indicator of breast cancer survival. Cancer Discov. 2011 Jun;1(1):54-67.

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