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XL228
🥰Excellent
Catalog No. T17267Cas No. 898280-07-4
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).
XL228
🥰Excellent
Purity: 99.07%
Catalog No. T17267Cas No. 898280-07-4
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $51 | In Stock | |
| 2 mg | $71 | In Stock | |
| 5 mg | $101 | In Stock | |
| 10 mg | $152 | In Stock | |
| 25 mg | $271 | In Stock | |
| 50 mg | $413 | In Stock | |
| 100 mg | $613 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $112 | In Stock |
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Purity:99.07%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Smiles | CC(C)c1cc(CNc2nc(Nc3cc([nH]n3)C3CC3)cc(n2)N2CCN(C)CC2)on1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 83.33 mg/mL (190.45 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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