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CEP-28122 mesylate salt
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CEP-28122 mesylate salt图片
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
CEP-28122甲磺酸盐是一种高度有效的选择性ALK抑制剂, IC50值为1.9 ± 0.5 nM。
Canonical SMILESO=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
分子式C29H39ClN6O6S
分子量635.17
溶解度DMSO: ≥ 6.4 mg/mL (10.08 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CEP-28122 mesylate salt is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.IC50 value: 1.9 ± 0.5 nMTarget: ALKin vitro: CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 with IC50 of 46 ±10 nM. CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small celllung cancer (NSCLC), and neuroblastoma cells. [1]in vivo: CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher. [1]

[1]. Cheng M, et al. CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2012 Mar;11(3):670-679.