MPC-3100
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.
MPC-3100是基于嘌呤的Hsp90抑制剂,IC50值为60 nM[1]。
MPC-3100靶向Hsp90 N端的ATP结合位点,阻断ATP酶的活性。在Her2荧光素酶降解实验中,MPC-3100减少Hsp90的该客户蛋白,IC50值为60 nM。在HCT-116细胞系中,MPC-3100抑制细胞增殖,IC50值为540 nM。此外,MPC-3100在不同的癌细胞系,如NCI-N87 和DU-145中具有广谱的抗增殖活性。在NCI-N877胃癌异种移植模型中,MPC-3100也抑制肿瘤生长。而且,PK研究表明,MPC-3100具有良好的口服PK特性、良好的整体暴露和合理的肝清除率。I期临床研究表明,MPC-3100在低于600 mg/day剂量时是安全和耐受的[1]。
参考文献:
[1] Kim SH, Bajji A, Tangallapally R, Markovitz B, Trovato R, Shenderovich M, Baichwal V, Bartel P, Cimbora D, McKinnon R, Robinson R, Papac D, Wettstein D, Carlson R, Yager KM. Discovery of (2S)-1-[4-(2-{6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl}e
-thyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a purine-based Hsp90 inhibitor. J Med Chem. 2012 Sep 13;55(17):7480-501.
Storage | Store at -20°C |
M.Wt | 549.4 |
Cas No. | 958025-66-6 |
Formula | C22H25BrN6O4S |
Solubility | Soluble in DMSO |
Chemical Name | (2S)-1-[4-[2-[6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]purin-9-yl]ethyl]piperidin-1-yl]-2-hydroxypropan-1-one |
SDF | Download SDF |
Canonical SMILES | CC(C(=O)N1CCC(CC1)CCN2C3=C(C(=NC=N3)N)N=C2SC4=C(C=C5C(=C4)OCO5)Br)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。 |