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LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

| 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 B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF. |
| Targets&IC50 | p38α:2.1 μM (IC50), Abl-1:4.9 μM (IC50), ARAF:6.4 nM (IC50), BRAF:0.21 nM (IC50), Raf:0.072 nM (IC50) |
| 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] |
| Molecular Weight | 502.49 |
| Formula | C25H25F3N4O4 |
| Cas No. | 1800398-38-2 |
| Smiles | Cc1ccc(NC(=O)c2ccnc(c2)C(F)(F)F)cc1-c1cc(OCCO)nc(c1)N1CCOCC1 |
| Relative Density. | 1.353 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 15 mg/mL (29.85 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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