XL228 |
| カタログ番号GC13102 |
チロシンキナーゼ阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 898280-07-4
Sample solution is provided at 25 µL, 10mM.
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XL228, a tyrosine kinase inhibitor, is involved in binding to and inhibiting the activities of multiple tyrosine kinases, such as the insulin-like growth factor 1 receptor (IGF1R), Src tyrosine kinase, and Bcr-Abl tyrosine kinase. Blockade of these kinases may result in the inhibition of tumor angiogenesis, cell proliferation, and metastasis [1]. XL228 is a multitargeted protein kinase inhibitor targeting IGF1R, the aurora kinases, IGF-1R, cSrc, BCR/Abl and SRC kinases [2].
In vitro: XL228(5-100 nM) reduced cell survival by 10-70% in a dose and time dependent manner and inhibited migration and invasion of two tumors with high propensity to metastasize, FaDu and H460. Treatment with 50 and 100 nM XL228 abolished the ability of H460, A549 and FaDu cells to form colony. At 10 nM, XL228 significantly increased the radiosensitivity of H460, A549 and FaDu cells by enhancement factors (EF, at the survival fraction of 0.5) of 1.52, 1.31 and 1.67 respectively. But, In HN-5 cells, sensitization occurred only at 100 nM (EF = 2.27). In HN-5 cells, XL228 (100 nM)incubation induced accumulation of cells at the radiation sensitive G2/M phase of the cell cycle and induced apoptosis in 32% of cells [2].
Clinical trial: In a phase I study in patients with solid tumors or hematologic malignancies, XL228 showed a manageable toxicity profile and biological activity through decrease in target pathway and alternations in tumor nuclei [3].
References:
[1] Smith D C, Britten C, Garon E B. A phase I study of XL228, a multitargeted protein kinase inhibitor, in patients with solid tumors or multiple myeloma[J]. J ClinOncol, 2010, 28(15s suppl: abstr 3105).
[2] Matsumoto F, Molkentine D, Clary D O, et al. A multi-kinase inhibitor, XL228, enhanced human cancer cell radiosensitivity and suppressed cell invasion and migration[J]. Cancer Research, 2011, 71(8 Supplement): 2487-2487.
[3] Smith D C, Britten C, Clary D O, et al. A phase I study of XL228, a potent IGF1R/AURORA/SRC inhibitor, in patients with solid tumors or hematologic malignancies[J]. J ClinOncol, 2009, 27(15 suppl): 149s.
| Cas No. | 898280-07-4 | SDF | |
| Chemical Name | 4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine | ||
| Canonical SMILES | CC(C)C1=NOC(=C1)CNC2=NC(=CC(=N2)NC3=NNC(=C3)C4CC4)N5CCN(CC5)C | ||
| Formula | C22H31N9O | M.Wt | 437.54 |
| 溶解度 | ≥ 21.9 mg/mL in DMSO, ≥ 27.6 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2855 mL | 11.4275 mL | 22.8551 mL |
| 5 mM | 0.4571 mL | 2.2855 mL | 4.571 mL |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2855 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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