Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 51.00 | |
2 mg | In stock | $ 71.00 | |
5 mg | In stock | $ 101.00 | |
10 mg | In stock | $ 152.00 | |
25 mg | In stock | $ 271.00 | |
50 mg | In stock | $ 413.00 | |
100 mg | In stock | $ 613.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 112.00 |
Description | XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively). |
Targets&IC50 | Aurora A:3.1 nM, IGF-1R:1.6 nM |
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 [2][3]. |
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 [3]. |
Molecular Weight | 437.54 |
Formula | C22H31N9O |
CAS No. | 898280-07-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 83.33 mg/mL (190.45 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
XL228 898280-07-4 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Tyrosine Kinase/Adaptors IGF-1R Bcr-Abl Src Aurora Kinase Inhibitor XL 228 XL-228 inhibit inhibitor