CEP-28122
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 1.9 nM: blocks anaplastic lymphoma kinase (ALK).
CEP-28122, a highly potent, selective, orally bioavailable inhibitor of ALK, dampens the phosphorylation of ALK and ALK substrates in cells and triggers cytotoxicity or growth inhibition of ALK-positive cancer cells with a favorable pharmaceutical and pharmacokinetic profile and selective pharmacologic efficacy. CEP-28122 blocks ALK tyrosine phosphorylation in tumor xenografts in mice. ALK, which is constitutively activated in many human cancer types because of point mutations, gene amplification, and chromosomal translocations, has emerged as an excellent molecular target for cancer therapy.
In vitro: CEP-28122, concentration-dependently, triggered growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL) via inhibiting nucleophosmin (NPM) -ALK tyrosine (664) phosphorylation. Due to the CEP-28122 treatment, EML4-ALK tyrosine phosphorylation was blocked in non-small cell lung cancer (NSCLC) NCI-H2228 and NCI-H3122 cells and full-length ALK receptor tyrosine phosphorylation was inhibited in neuroblastoma cell line NB-1 cells [1].
In vivo: Severe combined immunodeficient (SCID) mice bearing Sup-M2 (B) or nu/nu mice bearing colon carcinoma HCT-116 (C) subcutaneous tumor xenografts were administered orally with CEP-28122 at 3, 10, or 30 mg/kg for 24 days. CEP-28122 showed inhibition of ALK tyrosine phosphorylation in a dose-dependent manner in tumor xenografts in mice when treated at 30 mg/kg. Moreover, CEP-28122 displayed dose-dependent antitumor activity in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice when administered orally at 30 mg/kg or higher [1].
Reference:
[1]. Cheng, M., Quail, M., Gingrich, D., Ott, G., Lu, L., & Wan, W. 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. Molecular Cancer Therapeutics. 2011; 11(3): 670-679.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 539.1 |
Cas No. | 1022958-60-6 |
Formula | C28H35ClN6O3 |
Solubility | ≤30mg/ml in DMSO;12mg/ml in dimethyl formamide |
Chemical Name | (1S,2S,3R,4R)-3-[[5-chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-bicyclo[2.2.1]hept-5-ene-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | COC1=C(NC2=NC=C(Cl)C(N[C@@H]3[C@H](C4)C=C[C@H]4[C@@H]3C(N)=O)=N2)C=CC5=C1CC[C@@H](N6CCOCC6)CC5 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |