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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), Raf:0.072 nM (IC50), BRAF: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) |
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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