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Cat. No. M10152
Naporafenib Structure


Size Price Availability
10mg USD 310  USD310 4-7 Days
25mg USD 540  USD540 4-7 Days
50mg USD 940  USD940 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Naporafenib (also known as LXH254) is an orally available inhibitor of C-Raf and B-Raf with potential antineoplastic activity. Naporafenib (LXH254) has demonstrated anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling. Moreover, LXH254 is a Type 2 ATP -competitive inhibitor of both B-Raf and C-Raf that keeps the kinase pocket in an inactive conformation, thereby reducing the paradoxical activation seen with many B-Raf inhibitors, and blocking mutant RAS-driven signaling and cell proliferation. 

Naporafenib (LXH254) exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes. Treatment with Naporafenib (LXH254) generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 502.49
Formula C25H25F3N4O4
CAS Number 1800398-38-2
Purity >99%
Solubility DMSO ≥ 90 mg/mL
Storage at -20°C

[1] Kelli-Ann Monaco, et al. Clin Cancer Res. LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors

[2] Siyeon Park, et al. Cancer Lett. Combined blockade of polo-like kinase and pan-RAF is effective against NRAS-mutant non-small cell lung cancer cells

[3] Marcelo V Negrao, et al. J Thorac Oncol. Molecular Landscape of BRAF-Mutant NSCLC Reveals an Association Between Clonality and Driver Mutations and Identifies Targetable Non-V600 Driver Mutations

[4] Shubham Atal, et al. J Clin Pharm Ther. Recent advances in targeted small-molecule inhibitor therapy for non-small-cell lung cancer-An update

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Keywords: Naporafenib, LXH254 supplier, Raf, inhibitors

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