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LXH254

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Catalog No. T11898Cas No. 1800398-38-2

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

LXH254

LXH254

🥰Excellent
Purity: 99.92%
Catalog No. T11898Cas No. 1800398-38-2
LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.
Pack SizePriceAvailabilityQuantity
1 mg$48In Stock
5 mg$124In Stock
10 mg$195In Stock
25 mg$382In Stock
50 mg$597In Stock
100 mg$726In Stock
200 mg$997In Stock
500 mg$1,520In Stock
1 mL x 10 mM (in DMSO)$137In Stock
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Purity:99.92%
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight502.49
FormulaC25H25F3N4O4
Cas No.1800398-38-2
SmilesCc1ccc(NC(=O)c2ccnc(c2)C(F)(F)F)cc1-c1cc(OCCO)nc(c1)N1CCOCC1
Relative Density.1.353 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.9901 mL9.9504 mL19.9009 mL99.5045 mL
5 mM0.3980 mL1.9901 mL3.9802 mL19.9009 mL
10 mM0.1990 mL0.9950 mL1.9901 mL9.9504 mL
20 mM0.0995 mL0.4975 mL0.9950 mL4.9752 mL

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