Pexidartinib (PLX3397; Turalio; CML261; FP113)

Alias: Pexidartinib; CML-261; FP-113; PLX3397; PLX 3397; CML 261; CML261; PLX-3397;FP 113; FP113; trade name: Turalio

Cat No.:V0630 Purity: =99.31%

COA Product Data Instructions for use SDS

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.

Pexidartinib (PLX3397; Turalio; CML261; FP113) Chemical Structure CAS No.: 1029044-16-3
Product category: c-Kit

This product is for research use only, not for human use. We do not sell to patients.

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ADD TO CART CHECKOUT BULK INQUIRY

1-708-310-1919 [email protected]

Other Forms of Pexidartinib (PLX3397; Turalio; CML261; FP113):

Pexidartinib HCl

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data
Related Products

Product Description

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.

Biological Activity I Assay Protocols (From Reference)

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)
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.
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].
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.
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 SelectScreen^TM profiling service provided the IC50 data.
Animal Protocol	MMTV-PyMT mice 40 mg/kg/day p.o.
References	[1]. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 2011 Jun;1(1):54-67. [2]. Microglia increases the proliferation of retinal precursor cells during postnatal development. Mol Vis. 2018 Jul 30;24:536-545. eCollection 2018. [3]. A phase I study of pexidartinib, a colony-stimulating factor 1 receptor inhibitor, in Asian patients with advanced solid tumors. Invest New Drugs. 2019 Mar 2. [4]. The CSF1 receptor inhibitor pexidartinib (PLX3397) reduces tissue macrophage levels without affecting glucose homeostasis in mice. Int J Obes (Lond). 2020;44(1):245-253.

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

Physicochemical Properties

Molecular Formula

C20H15CLF3N5

Molecular Weight

417.81

Exact Mass

417.10

Elemental Analysis

C, 57.49; H, 3.62; Cl, 8.49; F, 13.64; N, 16.76

CAS #

1029044-16-3

Related CAS #

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

Appearance

Yellow solid powder

SMILES

C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F

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)

Chemical Name

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

Synonyms

Pexidartinib; CML-261; FP-113; PLX3397; PLX 3397; CML 261; CML261; PLX-3397;FP 113; FP113; trade name: Turalio

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

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

(Please use freshly prepared in vivo formulations for optimal results.)

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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

Calculate Reset

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.

Note： (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.

Clinical Trial Information

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

Biological Data

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.