Naporafenib (LXH254)

Catalog No.S8745 Batch:S874502

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Technical Data

Formula

C25H25F3N4O4
Molecular Weight 502.49 CAS No. 1800398-38-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (199.0 mM)
Ethanol 100 mg/mL (199.0 mM)
Water 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 Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.
Targets
B-Raf [1] C-Raf [1]
In vitro

LXH254 not only inhibits MAPK signaling activity in tumor models harboring BRAFV600 mutation, but also inhibits mutant N- and KRAS-driven signaling due to its ability to inhibit both RAF monomers and dimers with similar potencies. LXH254 is orally bioavailable, demonstrates a direct PK/PD relationship and causes tumor regression in multiple cell line and primary human tumor derived xenograft models at well-tolerated doses[1].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Ku-19-19 cells

  • Concentrations

    2 μM

  • Incubation Time

    3 days

  • Method

    For crystal violet staining experiments, cells were seeded in 6-well plates at 50,000 to 100,000 cells/well for 3-day experiments and vehicle or drug (diluted in media) was added the day after plating.
Animal Study:

[2]
  • Animal Models

    Female athymic nude mice

  • Dosages

    30 mg/kg

  • Administration

    i.p.

Selleck's Naporafenib (LXH254) has been cited by 6 publications

BRAFΔβ3-αC in-frame deletion mutants differ in their dimerization propensity, HSP90 dependence, and druggability [ Sci Adv, 2023, 9(35):eade7486] PubMed: 37656784
RAF1 amplification drives a subset of bladder tumors and confers sensitivity to MAPK-directed therapeutics [ J Clin Invest, 2021, e147849] PubMed: 34554931
RAF1 amplification drives a subset of bladder tumors and confers sensitivity to MAPK-directed therapeutics [ J Clin Invest, 2021, e147849] PubMed: 34554931
Pan-RAF inhibitor LY3009120 is highly synergistic with low-dose cytarabine, but not azacitidine, in acute myeloid leukemia with RAS mutations [ Oncol Lett, 2021, 22(5):745] PubMed: 34539849
Durable Suppression of Acquired MEK Inhibitor Resistance in Cancer by Sequestering MEK from ERK and Promoting Anti-Tumor T-cell Immunity [ Cancer Discov, 2020, CD-20-0873] PubMed: 33318037
Combined blockade of polo-like kinase and pan-RAF is effective against NRAS-mutant non-small cell lung cancer cells [ Cancer Lett, 2020, 495:135-144] PubMed: 32979462

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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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