CCT128930 HCl
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.
CCT128930 HCl是一种强效的、选择性的、新型的和ATP竞争性的AKT2抑制剂(IC50= 6 nM)。CCT128930 HCl的选择性分别高于PKA激酶(IC50=168 nM)和p70S6K (IC50=120 nM)28倍和20倍。
Akt (蛋白激酶B)是丝氨酸/苏氨酸特异性蛋白激酶，在多种细胞过程中起重要作用，例如葡萄糖代谢、细胞凋亡、细胞增殖、转录和细胞迁移。
在多肿瘤细胞系中，CCT128930 HCl 显示抑制细胞增殖作用，并阻断不同Akt底物的磷酸化。在PTEN缺乏的人类胶质瘤细胞(U87MG)中，CCT128930 HCl治疗导致与Akt 途径抑制有关的G1期停滞。[ 1 ]
在U87MG 肿瘤异种移植物中，CCT128930 HCl抑制Akt下游生物标志物的磷酸化。在U87MG、HER-2阳性和IK3CA-突变的BT474人类乳腺癌异种移植物中，随着肿瘤体积减少，记录到抗肿瘤活性。接受CCT128930 HCl治疗的小鼠体外触须毛囊及离体处理的人类毛囊发生明显的pThr246 PRAS40减少。[ 1 ]
参考文献：
1. Yap TA, Walton MI, Hunter LJ et al. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Mol Cancer Ther. 2011 Feb;10(2):360-71.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 378.30 |
| Cas No. | 885499-61-6 (free base) |
| Formula | C18H21Cl2N5 |
| Solubility | insoluble in H2O; ≥17.1 mg/mL in DMSO; ≥5.17 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC=C(C=C1)CC2(CCN(C3=NC=NC4=C3C=CN4)CC2)N.Cl |
| 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。 |
| Description | CCT128930 HCl是一种强效的、ATP竞争性的和选择性的Akt2抑制剂，IC50值为6 nM。 | |||||
| 靶点 | Akt2 | p70 S6K | PKA | |||
| IC50 | 6 nM | 120 nM | 168 nM | |||
质量控制和MSDS
- 批次:
化学结构
