Free shipping on all orders over $ 500

Naporafenib

Cat. No. M10152
Naporafenib Structure
Synonym:

LXH254

Size Price Availability
10mg USD 310  USD310 4-7 Days
25mg USD 540  USD540 4-7 Days
50mg USD 940  USD940 4-7 Days
Free Delivery on orders over USD 500 Bulk Inquiry?

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
References

[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

Related Raf Products
AZ304

AZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF with IC50 values of 79 nM and 38 nM respectively.

Lifirafenib (BGB-283)

Lifirafenib (BGB-283) is a novel potent and selective RAF Kinase and EGFR inhibitor with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.

BI 882370

BI 882370 is a highly potent and selective RAF inhibitor that binds to the DFG-out (inactive) conformation of the BRAF kinase.

B-Raf inhibitor 1

B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 µM and 2 nM for A375 proliferation and A375 p-ERK, respectively.

PLX7904

PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Naporafenib, LXH254 supplier, Raf, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.