LY2874455

SKU: orb1305596

Description

LY2874455 is a potent pan-FGFR inhibitor investigated in preclinical and clinical studies for advanced cancers. It has demonstrated activity in both in vitro cellular assays and in vivo tumor models targeting FGFR-driven malignancies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1254473-64-7
• MW: 444.31
• Purity: 99.46% (May vary between batches)
• Formula: C₂₁H₁₉Cl₂N₅O₂
• SMILES: C[C@@H](Oc1ccc2[nH]nc(\C=C\c3cnn(CCO)c3)c2c1)c1c(Cl)cncc1Cl
• Target: VEGFR,FGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.43 mM);DMSO:82 mg/mL (184.56 mM);Ethanol:53 mg/mL (119.29 mM)

Bioactivity

• Target IC50:
  FGFR3:6.4 nM|FGFR4:6 nM|FGFR1:2.8 nM|FGFR2:2.6 nM|VEGFR2:7 nM
• In Vivo:
  LY2874455 exhibits FGFR-dependent anti-proliferative effects in KMS-11, OPM-2, SNU-16, and KATO-III cells. In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activity.
• In Vitro:
  In mice carrying xenografts of RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460, LY2874455 (3 mg/kg, orally administered) demonstrated dose-dependent inhibition of tumor growth. Additionally, LY2874455 effectively inhibited FGF-induced Erk phosphorylation in mouse cardiac tissue, with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively.
• Cell Research:
  Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). (Only for Reference)

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

Inhibitor, FGFR4, FGFR3, FGFR, FGFR1, FGFR2, Fibroblast growth factor receptor, LY 2874455, LY-2874455, LY2874455, inhibit, VEGFR2

Compound Identifiers

PubChem CID

46944259