CPI-1205
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.
生化IC50为0.002 μM,细胞EC50为0.032 μM。
CPI-1205是一种EZH2抑制剂。
Polycomb抑制复合体2(PRC2)通过在组蛋白3的赖氨酸27上进行甲基化标记在转录沉默中起关键作用。PRC2功能失调涉及某些恶性肿瘤和不良预后。因此,EZH2代表用于药理学干预的有希望的候选肿瘤学靶点。
体外:据先前的研究报道,在多发性骨髓瘤和浆细胞瘤细胞模型中,CPI-1205治疗引起细胞凋亡。对30种其它组蛋白或DNA甲基转移酶进行测试时,CPI-1205还具有清晰的选择性特征。此外,在对与EZH2高度相关的甲基转移酶EZH1进行测试时,CPI-1205显示出适度的选择性[1]。
体内:在动物研究中,在携带肿瘤的雌性CB-17 SCID小鼠中,CPI-1205以160 mg/kg剂量每天两次口服给药,持续25天。通过用CPI-1205治疗荷瘤小鼠,在两周内观察到肿瘤消退。到第25天结束时,记录显著的肿瘤生长抑制。未观察到显著的体重减轻,表明CPI-1205对于重复给药是良好耐受的。此外,第25天最后给药1小时后的血浆和肿瘤的分析显示出足够的血浆和肿瘤组织浓度[1]。
临床试验:在B细胞淋巴瘤患者中评估CPI-1205的研究目前正在招募参与者[2]。
参考文献:
[1] Vaswani RG et al. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas. J Med Chem.2016 Nov 10;59(21):9928-9941.
[2] https://clinicaltrials. gov/ct2/show/NCT02395601term=CPI-1205&rank=1.
Storage | Store at -20°C |
M.Wt | 518.57 |
Cas No. | 1621862-70-1 |
Formula | C27H33F3N4O3 |
Solubility | Soluble in DMSO |
Chemical Name | (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | CC1=CC(OC)=C(CNC(C2=C(C)N([C@H](C)C3CCN(CC(F)(F)F)CC3)C4=C2C=CC=C4)=O)C(N1)=O |
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。 |
质量控制和MSDS
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