CC-223
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为16 nM。
CC-223是一种口服有效的mTOR抑制剂。
MTOR途径对肿瘤发展至关重要,mTOR抑制剂表现出适度效果。
体外:经鉴定,CC-223是mTOR激酶的一种ATP竞争性抑制剂,靶向4EBP1和p70 S6激酶1的mTORC1以及mTORC2,阻止AKT磷酸化上调。此外,CC-223对mTOR激酶选择性有效,与相关脂质激酶PI3Ka相比显示出超过150倍的敏感性。此外,CC-223在许多非霍奇金淋巴瘤细胞系和实体瘤细胞系(例如包括神经胶质瘤、乳腺癌、肝细胞癌以及非小细胞肺癌)中有活性[1]。
体内:在动物研究中,选择CC-223用于评估在载有PC-3肿瘤的小鼠模型中的效力。用载体或多种剂量的CC-223每天一次口服治疗小鼠21天,或以5 mL / kg的剂量每天两次口服治疗小鼠21天,并在给药的最后一天测量最终减少的肿瘤体积。结果显示,所有CC-223在PC-3模型中具有剂量和时间表依赖性的肿瘤生长抑制。此外,观察到的CC-223最大效力测定为87%,在其耐受剂量为25 mg / kg q.d时获得。[1]。
临床试验:在先前的临床研究中发现,CC-223是可耐受的,具有可控的毒性。此外,还观察到初步抗肿瘤活性,如肿瘤消退和mTORC1/mTORC2途径抑制的证据[2]。
参考文献:
[1] Mortensen DS, et al. Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223. J Med Chem. 2015 Jul 9;58(13):5323-5333.
[2] Bendell JC, et al. A phase I dose-escalation study to assess safety, tolerability, pharmacokinetics, and preliminary efficacy of the dual mTORC1/mTORC2 kinase inhibitor CC-223 in patients with advanced solid tumors or multiple myeloma. Cancer.2015 Oct 1;121(19):3481-90.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 397.47 |
Cas No. | 1228013-30-6 |
Formula | C21H27N5O3 |
Solubility | insoluble in H2O; ≥108 mg/mL in DMSO; ≥20.28 mg/mL in EtOH |
Chemical Name | 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((1r,4r)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1N([C@H]2CC[C@H](OC)CC2)C3=NC(C4=CN=C(C(O)(C)C)C=C4)=CN=C3NC1 |
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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