CEP-28122 mesylate hydrochloride
CEP-28122 mesylate hydrochloride, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate hydrochloride has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate hydrochloride can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells.
For research use only. We do not sell to patients.
- CAS No.: 1354545-57-5
- Formula: C29H40Cl2N6O6S
- Molecular Weight:671.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
CEP-28122 (3-3000 nM; 48 hours) mesylate hydrochloride treatment leads to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture, associates with concentration-related caspase 3/7 activation[1]. CEP-28122 (30-1000 nM; 2 hours) mesylate hydrochloride treatment leads to substantial suppression of phosphorylation of putative downstream effectors of ALK in Sup-M2 cells, indicating that the downstream signaling pathways are mediated by individual ALK fusion protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Karpas-299, Sup-M2, Toledo and HuT-102 cells
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Concentration:10 nM, 100 nM, 1000 nM, 10000 nM
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Incubation Time:48 hours
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Result:Treatment led to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture.
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Cell Line:Sup-M2 cells
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Concentration:30 nM, 100 nM, 300 nM, 1000 nM
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Incubation Time:2 hours
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Result:Resulted in substantial suppression of phosphorylation of putative downstream effectors of ALK, including Stat-3, Akt, and ERK1/2 in Sup-M2 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SCID mice bearing Sup-M2 subcutaneous tumor xenografts and nu/nu mice bearing HCT116 aged 6-8 week old[1]
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Dosage:3 mg/kg, 10 mg/kg and 30 mg/kg
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Administration:oral gavage; twice a day; 12 days
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Result:Produced dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice. Had no antitumor activity in nu/nu mice bearing HCT116.
Chemical Information
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CAS No. 1354545-57-5
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Molecular Weight 671.64
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Formula C29H40Cl2N6O6S
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SMILES
O=C([C@H]1[C@](C2)([H])C=C[C@]2([H])[C@H]1NC3=NC(NC4=CC=C5C(CC[C@@H](N6CCOCC6)CC5)=C4OC)=NC=C3Cl)N.O=S(C)(O)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CEP-28122 mesylate hydrochloride Related Classifications
HY-18030B Related Classifications
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