(±)-Nutlin-3
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.
(±)-Nutlin-3是一种有效的和选择性的MDM2拮抗剂,IC50值为0.09 μM [1]。
Mouse double minute 2 homolog(MDM2)是一种重要的p53(肿瘤抑制子)负调节子。扰乱p53-MDM2的相互作用可以导致p53活化及肿瘤生长抑制。
(±)-Nutlin-3是一种有效的和选择性的MDM2拮抗剂。在正常和白血病B细胞中,Nutlin-3以剂量依赖的方式诱导p53蛋白积累。在B-CLL细胞中,Nutlin-3也诱导细胞死亡,IC50值为10.4 μM。Nutlin-3诱导p53靶基因的转录,如PCNA、CDKN1A/p21、GDF15、TNFRSF10B/TRAIL-R2、TP53I3/PIG3、GADD45和DDB1[2]。
在皮下接种人癌症异种移植物(SJSA-1)的小鼠中,Nutlin-3(200 mg/kg)每天两次口服给药,给药20天可抑制90%的肿瘤生长[1]。在携带UKF-NB-3rDOX20异种移植物的小鼠中,Nutlin-3(200 mg/kg)增加caspase-3的活性,并诱导细胞凋亡[3]。
参考文献:
1. Shinohara T, Uesugi M. In-vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Tanpakushitsu Kakusan Koso. 2007 Oct;52(13 Suppl):1816-7.
2. Secchiero P, Barbarotto E, Tiribelli M, et al. Functional integrity of the p53-mediated apoptotic pathway induced by the nongenotoxic agent nutlin-3 in B-cell chronic lymphocytic leukemia (B-CLL). Blood. 2006 May 15;107(10):4122-9.
3. Van Maerken T, Ferdinande L, Taildeman J, et al. Antitumor activity of the selective MDM2 antagonist nutlin-3 against chemoresistant neuroblastoma with wild-type p53. J Natl Cancer Inst. 2009 Nov 18;101(22):1562-74.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 581.49 |
Cas No. | 548472-68-0 |
Formula | C30H30Cl2N4O4 |
Solubility | ≥50.1 mg/mL in DMSO; ≥50.7 mg/mL in EtOH; insoluble in H2O |
Chemical Name | 4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=C(C=C1)C2N(C(N(C3)CCNC3=O)=O)C(C(C=CC(OC)=C4)=C4OC(C)C)=NC2C(C=C5)=CC=C5Cl |
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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