MI-77301 (SAR405838)
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.
MI-77301 (SAR405838) 是MDM2的特异性拮抗剂,Ki值为0.88 nM [1]。
Murine double minute 2(MDM2)是野生型p53的主要负向调节剂,p53是一种肿瘤抑制剂。MDM2是E3泛素连接酶,诱导p53降解,阻断p53的反式激活域(TAD)[1]。
MI-77301 (SAR405838) 是MDM2的拮抗剂。MI-77301 (SAR405838) 抑制SJSA-1、RS4;11、LNCaP和HCT-116肿瘤细胞系的生长,IC50值分别为0.092、0.089、0.27和0.20 μM。与其他细胞系相比,MI-77301 (SAR405838) 对于突变或缺失p53的癌细胞系表现出较高的选择性,对于HCT-116 (p53-/-)、SAOS-2、PC-3和SW620细胞系的IC50值分别为大于20 、大于10、大于10和大于10 μM [1]。
在异种移植SJSA-1、HCT-116、RS4;11和LNCaP肿瘤的小鼠中,MI-77301 (SAR405838) 以剂量和时间依赖性方式增加MDM2、p21和p53蛋白水平,诱导凋亡。在SJSA-1异种移植模型中,30-100 mg/kg 剂量的MI-77301 (SAR405838) 诱导肿瘤消退,显著抑制肿瘤生长[1]。
参考文献:
[1]. Wang S, Sun W, Zhao Y, et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res, 2014, 74(20): 5855-5865
Storage | Store at -20°C |
M.Wt | 562.50 |
Cas No. | 1303607-60-4 |
Formula | C29H34Cl2FN3O3 |
Solubility | ≥17.2 mg/mL in DMSO |
Chemical Name | (2'S,3R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-hydroxycyclohexyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide |
SDF | Download SDF |
Canonical SMILES | FC1=C(Cl)C=CC=C1[C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)[C@H](CC(C)(C)C)N[C@H]2C(N[C@@H]5CC[C@@H](O)CC5)=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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