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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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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.
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.
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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