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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 | Raf:0.072 nM (IC50), Abl-1:4.9 μM (IC50), ARAF:6.4 nM (IC50), p38α:2.1 μM (IC50), B-Raf:0.21 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. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.98 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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