GDC-0980 (RG7422)
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.
GDC-0980(RG7422)是一种选择性的、新型的、有效的1类PI3K / mTOR激酶的口服抑制剂,作用于mTOR激酶的Ki值为17 nmol/ L [1]。
在前列腺癌、乳腺癌和NSCLC细胞系中,GDC-0980(RG7422)已经显示出有效的抑制作用,IC50值小于200 nmol/ L。此外,研究表明,在KPL4细胞中,GDC-0980(RG7422)通过抑制细胞周期和诱导细胞凋亡来降低细胞活力,抑制细胞周期的IC50值为109 nM,诱导凋亡的EC50值为78 nM。口服GDC-0980(RG7422)显著抑制异种移植模型的肿瘤应答。值得注意的是,在体实验研究表明,GDC-0980(RG7422)和抗肿瘤剂docetaxel共同使用可以加强抗肿瘤活性[1]。
参考文献:?
[1] Wallin JJ1, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 498.61 |
Cas No. | 1032754-93-0 |
Formula | C23H30N8O3S |
Solubility | ≥21.35 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | (2S)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one |
SDF | Download SDF |
Canonical SMILES | CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)C(=O)C(C)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。 |
描述 | Apitolisib(GDC-0980,RG7422)是一种强效的I类PI3K抑制剂,作用于PI3Kα/β/δ/γ的IC50值分别是5 nM、27 nM、7 nM和14 nM。 | |||||
靶点 | p110α | p110δ | p110γ | mTOR | p110β | |
IC50 | 5 nM | 7 nM | 14 nM | 17 nM(Ki app) | 27 nM |
质量控制和MSDS
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