Description

Pexidartinib (PLX-3397) is a potent, orally active, and ATP-competitive inhibitor of colony stimulating factor 1 receptor (CSF1R/M-CSFR) and c-Kit, with IC₅₀ values of 20 nM and 10 nM, respectively. It displays 10- to 100-fold selectivity for CSF1R and c-Kit over related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and demonstrates strong anti-tumor activity in research models.

Specification

CAS No.	1029044-16-3
Synonyms	PLX3397
Molecular Formula	C₂₀H₁₅ClF₃N₅
Formula Weight	417.81
Purity	≥98%
Formulation	A crystalline solid
Solubility	DMF: 20 mg/ml DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml DMSO: 20 mg/ml
Color	Off-white to light yellow
SMILES	ClC1=CC2=C(N=C1)NC=C2CC3=CN=C(NCC4=CN=C(C(F)(F)F)C=C4)C=C3
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)
InChi Key	JGWRKYUXBBNENE-UHFFFAOYSA-N

Features

Dual Kinase Inhibitor: Potently inhibits CSF1R and c-Kit with nanomolar activity.
High Selectivity: Demonstrates strong selectivity over related kinases, reducing off-target effects in research assays.
XRD-Verified Crystal Form: Confirmed high-activity and high-stability crystalline form by X-ray diffraction.
Superior Reproducibility: Ensures consistent lot-to-lot performance and reliable experimental results.
High Purity: ≥99.5% purity by HPLC for precise and reproducible research applications.
Flexible Solubility: Soluble in DMSO and DMF, compatible with common in vitro and in vivo research protocols.

Applications

Oncology Research: Study tumor growth, apoptosis, and kinase-driven cancer pathways.
Immuno-Oncology Studies: Investigate CSF1R signaling and tumor-associated macrophage modulation.
Kinase Signaling Research: Explore CSF1R- and c-Kit-mediated signaling mechanisms.
Drug Discovery & Preclinical Research: Evaluate kinase inhibition efficacy and structure-activity relationships.
Cell-Based Assays: Assess anti-proliferative and pro-apoptotic effects in relevant cell models.

Crystal Form Verified by X-ray Diffraction (XRD)

PLX-3397 obtained from different suppliers can display different crystalline forms, which may lead to notable variations in biological activity, solubility, stability, and experimental reproducibility.

Biofargo’s PLX-3397 is confirmed by X-ray diffraction (XRD) to be a high-activity and highly stable crystal form, ensuring:

Consistent lot-to-lot performance
Highly reproducible experimental outcomes
Superior biological activity compared with non-verified crystal forms
Reliable solubility behavior across assays

For research use only. We do not sell to patients.

Documents

MSDS

COA

Pexidartinib (PLX3397) Purity 99.5%