XL228

SKU: orb1307597

Description

XL228

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 898280-07-4
• MW: 437.54
• Purity: 98.92%
• Formula: C₂₂H₃₁N₉O
• SMILES: CC(C)c1cc(CNc2nc(Nc3cc([nH]n3)C3CC3)cc(n2)N2CCN(C)CC2)on1
• Target: Src,Bcr-Abl,Aurora Kinase,IGF-1R
• Solubility: DMSO:83.33 mg/mL (190.45 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.54 mM)

Bioactivity

• Target IC50:
  Aurora A:3.1 nM|IGF-1R:1.6 nM
• In Vivo:
  Single-dose pharmacodynamics studies demonstrate that XL228 on BCR-ABL signaling in K562 xenograft tumors has a potent effect. At XL228 plasma concentrations of 3.5 μM, phosphorylation of BCR-ABL is decreased by 50%; a similar decrease in phospho-STAT5 occurred at 0.8 μM plasma concentration .
• In Vitro:
  XL228 inhibits phosphorylation of BCR-ABL and its substrate STAT5 in K562 cells in vitro (IC50s: 33 and 43 nM, respectively). XL228 eliminates the phosphorylation of Aurora A and B at concentrations above 10 nM. XL228 displays a broad pattern of protein kinase inhibition, including the tyrosine kinases IGF1R, SRC, ABL, FGFR1-3, and ALK and the serine/threonine kinases Aurora A and Aurora B. Approximately 30% of the lines demonstrate XL228 IC50 values of <100nM in viability assays, including many lines with characterized ALK or FGFR mutations or amplifications .

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

inhibit, Inhibitor, Lyn, IGF-1R, IGF1R, BcrAbl, Bcr-Abl, Aurora Kinase, AuroraKinase, Aurora A, Src, XL228, XL-228, XL 228

Compound Identifiers

PubChem CID

59757974