Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LXH254 is a potent C-Raf and B-Raf inhibitor.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 48.00 | |
5 mg | In stock | $ 124.00 | |
10 mg | In stock | $ 195.00 | |
25 mg | In stock | $ 382.00 | |
50 mg | In stock | $ 597.00 | |
100 mg | In stock | $ 726.00 | |
200 mg | In stock | $ 997.00 | |
500 mg | In stock | $ 1,520.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 137.00 |
Description | LXH254 is a potent C-Raf and B-Raf inhibitor. |
Targets&IC50 | BRAF:0.21 nM (IC50), Raf:0.072 nM (IC50), Abl-1:4.9 μM (IC50), ARAF:6.4 nM (IC50), p38α:2.1 μM (IC50) |
In vitro | LXH254 is an adenosine triphosphate (ATP)-competitive inhibitor of BRAF and CRAF protein kinases. 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. |
In vivo | 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 LXH254 generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C). |
Molecular Weight | 502.49 |
Formula | C25H25F3N4O4 |
CAS No. | 1800398-38-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (199.01 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
LXH254 1800398-38-2 MAPK Raf Bcr-Abl A375 Inhibitor p38 MAPK inhibit Mia PaCa-2 Raf kinases LXH-254 LXH 254 HCT116 Selective MEL-JUSO inhibitor