Plixorafenib (PLX8394)

Catalog No.S7965 Batch:S796503

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Technical Data

Formula

C25H21F3N6O3S
Molecular Weight 542.53 CAS No. 1393466-87-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (184.32 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Plixorafenib (PLX8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.
Targets
BRAF(V600E) [2]
(Cell-free assay)		 BRAF [2]
(Cell-free assay)		 CRAF [2]
(Cell-free assay)
3.8 nM 14 nM 23 nM
In vitro

PLX8394 is a next-generation, orally available small-molecule BRAFi that does not induce the RAF/MEK/ERK paradoxical activation and blocks signaling from both monomeric BRAFV600 and dimeric BRAFnon-V600 protein[1].
In vivo

PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with potential antineoplastic activity.

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    colorectal cancer cell lines

  • Concentrations

    1 μM

  • Incubation Time

    6 h

  • Method

    Cells were treated with DMSO, PLX8394 at 1 μM for 6 h.

Selleck's Plixorafenib (PLX8394) has been cited by 13 publications

Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936] PubMed: 38588697
Mcl-1 mediates intrinsic resistance to RAF inhibitors in mutant BRAF papillary thyroid carcinoma [ Cell Death Discov, 2024, 10(1):175] PubMed: 38622136
SB202190 Predicts BRAF-Activating Mutations in Primary Colorectal Cancer Organoids via Erk1-2 Modulation [ Cells, 2023, 12(4)664] PubMed: 36831331
SB202190 Predicts BRAF-Activating Mutations in Primary Colorectal Cancer Organoids via Erk1-2 Modulation [ Cells, 2023, 12(4)664] PubMed: 36831331
Design and Synthesis of Novel 2-Acetamido, 6-Carboxamide Substituted Benzothiazoles as Potential BRAFV600E Inhibitors - In vitro Evaluation of their Antiproliferative Activity [ ChemMedChem, 2023, e202300322.] PubMed: 37792577
Classical RAS proteins are not essential for paradoxical ERK activation induced by RAF inhibitors [ Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119] PubMed: 35091470
Increased IRF9-STAT2 signaling leads to adaptive resistance toward targeted therapy in melanoma by restraining GSDME-dependent pyroptosis [ J Invest Dermatol, 2022, S0022-202X(22)00096-3] PubMed: 35148998
Preclinical Characterization of a Next-Generation Brain Permeable, Paradox Breaker BRAF Inhibitor [ Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2761] PubMed: 34782366
Preclinical characterization of a next generation brain permeable, paradox breaker BRAF inhibitor [ Clin Cancer Res, 2021, clincanres.2761.2021] PubMed: 34782366
The stability of R-spine defines RAF inhibitor resistance: A comprehensive analysis of oncogenic BRAF mutants with in-frame insertion of αC-β4 loop [ Sci Adv, 2021, 7(24)eabg0390] PubMed: 34108213

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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