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100mg |
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250mg |
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500mg |
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1g |
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Purity: ≥98%
Pexidartinib (formerly PLX-3397; CML-261; FP-113; trade name Turalio) is a multi-targeted, orally bioavailable RTK (receptor tyrosine kinase) inhibitor of Flt3, Kit, and CSF-1R that may have anticancer effects. Its IC50s are 20 nM, 10 nM, and 160 nM for CSF-1R, Kit, and Flt3, respectively, and they are inhibitory. The FDA approved Pexidartinib in August 2019 to treat giant-cell tumors of the tendon sheath (GC-TS). However, the Turalio Risk Evaluation and Mitigation Strategy (REMS) Program is the only way to access it in the United States.
Targets |
FGFR1 (IC50 = 10 nM); cFMS (IC50 = 20 nM); FLT3 (IC50 = 160 nM); KDR (IC50 = 350 nM); LCK (IC50 = 860 nM); FLT1 (IC50 = 880 nM); NTRK3 (IC50 = 890 nM)
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ln Vitro |
Pexidartinib (PLX-3397) is an ATP-competitive, potent, and selective inhibitor of CSF1R (cFMS) and c-Kit that exhibits selectivity for c-Kit and CSF1R over other related kinases, FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1), and NTRK3 (TRKC), with IC50 values of 160, 350, 860, 880, and 890 nM, respectively.
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ln vivo |
Pexidartinib (PLX3397; 0.25, 1 mg/kg, twice daily for 8 days) prevents the growth of BrdU-positive cells and microglia in neonatal mice[2].
Pexidartinib (1 mg/kg, twice daily for 8 day) does not appear to have any noticeable effects on mice's cleaved caspase-3-positive cells[2].
Pexidartinib (50 mg/kg; p.o.; every second day for 3 weeks) lowers tissue macrophage counts in mice without changing the homeostasis of glucose[4].
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Enzyme Assay |
Pexidartinib (PLX-3397) is an ATP-competitive, potent, and selective inhibitor of CSF1R (cFMS) and c-Kit that exhibits selectivity for c-Kit and CSF1R over other related kinases, FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1), and NTRK3 (TRKC), with IC50 values of 160, 350, 860, 880, and 890 nM, respectively.
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Cell Assay |
PLX3397 is found to be a strong inhibitor of both CSF-1R and c-KIT kinase through the application of scaffold- and X-ray structure-based discovery methodology. The SelectScreenTM profiling service provided the IC50 data.
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Animal Protocol |
MMTV-PyMT mice
40 mg/kg/day p.o. |
References |
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Molecular Formula |
C20H15CLF3N5
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Molecular Weight |
417.81
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Exact Mass |
417.10
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Elemental Analysis |
C, 57.49; H, 3.62; Cl, 8.49; F, 13.64; N, 16.76
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CAS # |
1029044-16-3
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Related CAS # |
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Appearance |
Yellow solid powder
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SMILES |
C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F
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InChi Key |
JGWRKYUXBBNENE-UHFFFAOYSA-N
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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)
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Chemical Name |
5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine
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Synonyms |
Pexidartinib; CML-261; FP-113; PLX3397; PLX 3397; CML 261; CML261; PLX-3397;FP 113; FP113; trade name: Turalio
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3934 mL | 11.9672 mL | 23.9343 mL | |
5 mM | 0.4787 mL | 2.3934 mL | 4.7869 mL | |
10 mM | 0.2393 mL | 1.1967 mL | 2.3934 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02975700 | Active Recruiting |
Drug: PLX3397 | Melanoma | Daiichi Sankyo Co., Ltd. | January 2017 | Not Applicable |
NCT04488822 | Active Recruiting |
Drug: Pexidartinib | Tenosynovial Giant Cell Tumor | Daiichi Sankyo Co., Ltd. | September 25, 2020 | Phase 3 |
NCT04703322 | Recruiting | Drug: Pexidartinib | Tenosynovial Giant Cell Tumor | Daiichi Sankyo Co., Ltd. | March 15, 2021 | Phase 2 |
NCT04635111 | Recruiting | Drug: TURALIO™ | Hepatotoxicity Tenosynovial Giant Cell Tumor |
Daiichi Sankyo, Inc. | January 7, 2021 | |
NCT02390752 | Recruiting | Drug: Turalio | Sarcoma Neurofibroma, Plexiform |
National Cancer Institute (NCI) |
April 29, 2015 | Phase 1 |
Combined PLX3397 and PTX treatment inhibits metastasis in a CD8-dependent manner. Cancer Discov. 2011 Jun 1; 1: 54–67. |
PTX in combination with PLX3397 induces antitumor T-cell response. Cancer Discov. 2011 Jun 1; 1: 54–67. |
CD68/CD4/CD8 immune signature is an independent prognostic indicator of breast cancer survival. Cancer Discov. 2011 Jun;1(1):54-67. |