LXH254

SKU: orb1309463

Description

LXH254

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1800398-38-2
• MW: 502.49
• Purity: 99.92%
• Formula: C₂₅H₂₅F₃N₄O₄
• SMILES: Cc1ccc(NC(=O)c2ccnc(c2)C(F)(F)F)cc1-c1cc(OCCO)nc(c1)N1CCOCC1
• Target: Bcr-Abl,Raf,p38 MAPK
• Solubility: DMSO:125 mg/mL (248.76 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.98 mM)

Bioactivity

• Target IC50:
  ARAF:6.4 nM (IC50)|Abl-1:4.9 μM (IC50)|B-Raf:0.21 nM (IC50)|Raf:0.072 nM (IC50)|p38α:2.1 μM (IC50)
• 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.
• 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 . 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HCT116, MEL-JUSO, inhibit, Inhibitor, Mia PaCa-2, LXH 254, LXH254, LXH-254, C-Raf, c-Raf, B-Raf, Bcr-Abl, A375, Selective, p38 MAPK, Raf, Raf kinases

Compound Identifiers

PubChem CID

90456533