Naporafenib,1800398-38-2

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LXH254

CAS No. : 1800398-38-2

MCE 国际站：LXH254

产品活性：LXH254 是一种有效的、具有口服活性的 II 型 BRAF 和 CRAF 抑制剂，对 CRAF 和 BRAF的 IC₅₀ 值分别为 0.072 和 0.21 nM。

研究领域：MAPK/ERK Pathway  |  Protein Tyrosine Kinase/RTK

作用靶点：Raf  |  p38 MAPK  |  Bcr-Abl

In Vitro: LXH254 (Compound A) is an adenosine triphosphate (ATP)-competitive inhibitor of BRAF (also referred to herein as b-RAF or b-Raf) and CRAF (also referred to herein as c-RAF or c- Raf) protein kinases. Throughout the present disclosure, LXH254 is also referred to as a c-RAF (or CRAF) inhibitor or a C-RAF/c-Raf kinase inhibitor. In cell-based assays, 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.
LXH254 (0-10 µM, 1 h) inhibits both monomeric and dimeric RAF and promotes RAF dimer formation.
LXH254 has reduced ability to suppress MAPK signaling driven by ARAF and further that the contribution of ARAF to MAPK signaling increases in the absence of CRAF expression.
LXH254 shows more sensitivity when cells lack ARAF.

In Vivo: Treatment with LXH254 (Compound A) generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C). 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.
LXH254 shows significant antitumor activity in models harboring BRAF mutations either alone or coincident with either activated NRAS or KRAS, and RAS mutants lacking ARAF are more sensitive to LXH254.

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