| CEP-28122anaplastic lymphoma kinase (ALK) inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 1022958-60-6 | SDF | Download SDF |
| 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 | ||
| 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 | ||
| Formula | C28H35ClN6O3 | M.Wt | 539.1 |
| Solubility | ≤30mg/ml in DMSO;12mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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最近遇到了实验上的大问题，就是用一步法做RNA的荧光定量PCR时，发现低浓度的做不出来，而DNA是可以的，想请问各位在一步法PCR中有没有什么高见，就是逆转录的Buffer有没有什么需要注意的地方！就是在逆转录酶的最适Buffer和Taq酶的最适Buffer中寻找一个最适的Buffer！
DNA拓扑异构酶Ⅱ与抗肿瘤药物靶点的研究进展.doc(59.5k)
B、酶细胞产能细胞内（外）起作用消化酶细胞外起作用B错误；
C、酶同需要适条件同胃蛋白酶与胰蛋白酶所需PH同C错误；
D、葡萄糖细胞质基质解丙酮酸需要酶催化D确．
故选：D．
我是新手。我要开始做实验了，但一开始就碰到了个很大的问题。
我想买个能利用哺乳动物细胞RNA聚合酶将DNA转录成RNA的的质粒，向好几家公司打了电话，但都没有我想要的东西。
没有这个东西，我的实验就只能是蓝图了。哪位战友有办法的，能不能帮帮我？
不胜感激。
请规范发贴，求助贴请在标题前加【求助】，谢谢您的合作。——by草根
