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NSC348884 Sale

(Synonyms: N1,N1,N2,N2-四[(6-甲基-1H-苯并咪唑-2-基)甲基]-1,2-乙二胺) 目录号 : GC16151

A nucleophosmin inhibitor

NSC348884 Chemical Structure

Cas No.:81624-55-7

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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 1.7-4.0 μM for tested cancer cell lines

NSC348884 is a nucleophosmin inhibitor.

Nucleophosmin is identified as a multifunctional nucleolar phosphoprotein, which is dysregulated in human malignancies resulting in anti-apoptosis and differentiation inhibition.

In vitro: NSC348884, which was identified as a putative nucleophosmin small molecular inhibitor, was found to be able to disrupt a hydrophobic pocket that was required for oligomerization, and NSC348884 could also inhibit the cell proliferation in distinct cancer cell lines and disrupt nucleophosmin oligomer formation. Moreover, the treatment of several cancer cell types with NSC348884 could dose-dependently upregulate p53 and also induce apoptosis that correlated with H2AX phosphorylation, poly(ADP-ribose) polymerase cleavage as well as Annexin V. Furthermore, NSC348884 could also synergize doxorubicin cytotoxicity on the viability of cancer cells [1].

In vivo: Previous study showed that the in-vivo intravasation and invasion could be significantly inhibited after the injection of NSC348884 into the tumor-bearing mice. In addition, there was no significant difference in overall cell death that was observed by histology in the treated tumors with the 4-hour brief treatments, indicating that the inhibition seen was specific to migration [2].

Clinical trial: Up to now, NSC348884 is still in the preclinical development stage.

References:
[1] Qi W,Shakalya K,Stejskal A,Goldman A,Beeck S,Cooke L,Mahadevan D.  NSC348884, a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis in human cancer cells. Oncogene.2008 Jul 10;27(30):4210-20.
[2] Patsialou A,Wang Y,Lin J,Whitney K,Goswami S,Kenny PA,Condeelis JS.  Selective gene-expression profiling of migratory tumor cells in vivo predicts clinical outcome in breast cancer patients. Breast Cancer Res.2012 Oct 31;14(5):R139.

Chemical Properties

Cas No. 81624-55-7 SDF
别名 N1,N1,N2,N2-四[(6-甲基-1H-苯并咪唑-2-基)甲基]-1,2-乙二胺
化学名 N1,N1,N2,N2-tetrakis((6-methyl-1H-benzo[d]imidazol-2-yl)methyl)ethane-1,2-diamine
Canonical SMILES CC1=CC=C2N=C(CN(CC3=NC4=CC=C(C)C=C4N3)CCN(CC5=NC6=CC=C(C)C=C6N5)CC7=NC8=CC=C(C)C=C8N7)NC2=C1
分子式 C38H40N10 分子量 636.79
溶解度 ≥ 63.7mg/mL in DMSO 储存条件 Store at -20°C
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1 mM 1.5704 mL 7.8519 mL 15.7038 mL
5 mM 0.3141 mL 1.5704 mL 3.1408 mL
10 mM 0.157 mL 0.7852 mL 1.5704 mL
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