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Naporafenib

Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively[1][2].

Product Specifications

CAS Number

[1800398-38-2]

Product Name Alternative

LXH254

UNSPSC

12352005

Hazard Statement

H302

Target

Bcr-Abl; p38 MAPK; Raf

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LXH254.html

Purity

99.90

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=CC=C(NC(C2=CC(C(F)(F)F)=NC=C2)=O)C=C1C3=CC(N4CCOCC4)=NC(OCCO)=C3

Molecular Formula

C25H25F3N4O4

Molecular Weight

502.49

Precautions

H302

References & Citations

[1]CAPONIGRO, Giordano, et al. THERAPEUTIC COMBINATIONS COMPRISING A RAF INHIBITOR AND A ERK INHIBITOR. WO 2018051306 A1 20180322|[2]Kelli-Ann Monaco, et al. LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors. Clin Cancer Res. 2021 Apr 1;27 (7) :2061-2073.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

Abl; B-Raf; C-Raf; p38α

Available Sizes

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