CEP-28122
CEP-28122, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 has good pharmacodynamic and pharmacokinetic activity. CEP-28122 can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1022958-60-6
- 分子式: C28H35ClN6O3
- 分子量:539.07
-
保管条件:
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-299 | IC50 |
20 nM
Compound: 25b, diasteromer 2
|
Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma
Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma
|
[PMID: 22564207] |
CEP-28122 (3-3000 nM; 48 hours) 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) 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.
-
Cell Line:Karpas-299, Sup-M2, Toledo and HuT-102 cells
-
Concentration:10 nM, 100 nM, 1000 nM, 10000 nM
-
Incubation Time:48 hours
-
Result:Treatment led to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture.
-
Cell Line:Sup-M2 cells
-
Concentration:30 nM, 100 nM, 300 nM, 1000 nM
-
Incubation Time:2 hours
-
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.
-
Animal Model:Female SCID mice bearing Sup-M2 subcutaneous tumor xenografts and nu/nu mice bearing HCT116 aged 6-8 week old[1]
-
Dosage:3 mg/kg, 10 mg/kg and 30 mg/kg
-
Administration:oral gavage; twice a day; 12 days
-
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.
化学情報
-
CAS 番号 1022958-60-6
-
分子量 539.07
-
分子式 C28H35ClN6O3
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
-
データシート (274 KB)
-
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CEP-28122 関連分類
HY-18030 関連分類
Powered by Bioz