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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
5 mg | $124 | In Stock | |
10 mg | $195 | In Stock | |
25 mg | $382 | In Stock | |
50 mg | $597 | In Stock | |
100 mg | $726 | In Stock | |
200 mg | $997 | In Stock | |
500 mg | $1,520 | In Stock | |
1 mL x 10 mM (in DMSO) | $137 | In Stock |
Description | LXH254 is a potent C-Raf and B-Raf inhibitor. |
Targets&IC50 | ARAF:6.4 nM (IC50), BRAF:0.21 nM (IC50), p38α:2.1 μM (IC50), Raf:0.072 nM (IC50), Abl-1:4.9 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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 15 mg/mL (29.85 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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