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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 | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $51 | In Stock | In Stock | |
| 2 mg | $71 | In Stock | In Stock | |
| 5 mg | $101 | In Stock | In Stock | |
| 10 mg | $152 | In Stock | In Stock | |
| 25 mg | $271 | In Stock | In Stock | |
| 50 mg | $413 | In Stock | In Stock | |
| 100 mg | $613 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $112 | In Stock | In Stock |
| 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 | IGF-1R:1.6 nM, Aurora A:3.1 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 |
| Smiles | CC(C)c1cc(CNc2nc(Nc3cc([nH]n3)C3CC3)cc(n2)N2CCN(C)CC2)on1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 83.33 mg/mL (190.45 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.54 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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