PLX7904

Catalog No.S7964 Batch:S796402

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Technical Data

Formula

C24H22F2N6O3S
Molecular Weight 512.53 CAS No. 1393465-84-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (195.11 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5mg/ml (9.76mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.71mg/ml (1.39mM) Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

Biological Activity

Description PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.
Targets
Raf [1]
In vitro PLX7904 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Consistent with ERK1/2 re-activation driving the re-acquisition of malignant properties, this compound promotes apoptosis and inhibits entry into S phase and anchorage-independent growth in mutant N-RAS mediated vemurafenib-resistant cells. This chemical is also evaluated in the human SCC cell line A431 and the human breast adenocarcinoma cell line SKBR3 as these cells achieve MAPK pathway activation by upstream signals feeding into RAS (through overexpression of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), respectively).
In vivo PLX7904 inhibits the COLO205 xenograft growth in eight mice per group.

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    WM793, WM115, WM9, WM278, WM1346, WM1366, WM1361A, Sbcl2, 1205Lu, A375, SK-MEL 24, SKMEL-2, and SK-MEL 207 cells

  • Concentrations

    0, 0.5, 1, 5 μM

  • Incubation Time

    24 h

  • Method

    Cells are treated with PB04(PLX7904) at different concentrations (0, 0.05, 0.1, 1, 5 μM) for 24 h. Cells are lysed and analyzed by Western blotting with phospho-MEK1/2, total MEK1/2, phospho-ERK1/2 and total ERK1/2 antibodies.

References

  • https://pubmed.ncbi.nlm.nih.gov/26466569/
  • https://pubmed.ncbi.nlm.nih.gov/23490205/

Selleck's PLX7904 Has Been Cited by 17 Publications

A structure-based modelling approach identifies effective drug combinations for RAS-mutant acute myeloid leukemia [ bioRxiv, 2025, nan] PubMed: 40654850
Oncogenic BRAF induces whole-genome doubling through suppression of cytokinesis [ Nature Communications, 2022, 4109] PubMed: 35840569
Oncogenic BRAF induces whole-genome doubling through suppression of cytokinesis [ Nat Commun, 2022, 13(1):4109] PubMed: 35840569
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
A Cell-Based MAPK Reporter Assay Reveals Synergistic MAPK Pathway Activity Suppression by MAPK Inhibitor Combination in BRAF-Driven Pediatric Low-Grade Glioma Cells [ Molecular Cancer Therapeutics, 2020, 1736-1750] PubMed: 32451331
A Cell-Based MAPK Reporter Assay Reveals Synergistic MAPK Pathway Activity Suppression by MAPK Inhibitor Combination in BRAF-driven Pediatric Low-Grade Glioma Cells [ Mol Cancer Ther, 2020, 25;molcanther.1021.2019] PubMed: 32451331
Analyses of the oncogenic BRAFD594G variant reveal a kinase-independent function of BRAF in activating MAPK signaling [ Journal of Biological Chemistry, 2020, 2407-2420] PubMed: 31929109
Analyses of the oncogenic BRAFD594G variant reveal a kinase-independent function of BRAF in activating MAPK signaling. [ J Biol Chem, 2020, 295(8):2407-2420] PubMed: 31929109
Distinct Binding Preferences between Ras and Raf Family Members and the Impact on Oncogenic Ras Signaling. [ Mol Cell, 2019, 76(6):872-884] PubMed: 31606273
Fusion Kinases Identified by Genomic Analyses of Sporadic Microsatellite Instability-High Colorectal Cancers [ Clinical Cancer Research, 2019, 378-389] PubMed: 30279230

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.