| Name | LXH254 |
| Description | LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF. |
| In vitro | METHODS: HCT 116 cells were treated with LXH254 at 10 µM for 2 hours, and lysates were then processed, probe labeled, and analyzed by LC-MS/MS for intracellular kinase selectivity analysis using KiNativ™.
RESULTS LXH254 inhibited 80% of the kinases in HCT 116 cells [1]. METHODS: The sensitivity of WT cell lines to LXH254 was analyzed in a high-throughput format. Use IC50 values in the range 1-2.5 μM.
RESULTS LXH254 effectively inhibited RAF signaling in the insensitive model tested [1]. |
| In vivo | METHODS: The anti-tumor effects of LXH254 were tested in a set of BRAF, NRAS and KRAS mutant xenograft models as well as RAS/RAF wild-type models, treated with LXH254 100mgkg orally once daily for one month.
RESULTS LXH254 can inhibit the growth of tumor in model mice. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.98 mM), Sonication is recommended.
DMSO : 125 mg/mL (248.76 mM), Sonication is recommended.
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| Keywords | Selective | Raf kinases | Raf | p38 MAPK | Mia PaCa-2 | MEL-JUSO | LXH-254 | LXH254 | LXH 254 | Inhibitor | inhibit | HCT116 | C-Raf | B-Raf | Bcr-Abl | A375 |
| Inhibitors Related | Undecane | Esculin | Bisphenol A | Fumaric acid | Sorafenib | Dasatinib | Regorafenib | Dabrafenib | Skatole | Afatinib | FERULIC ACID METHYL ESTER | (Rac)-Hesperetin |
| Related Compound Libraries | Highly Selective Inhibitor Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
