NSC745885

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NSC745885  纯度: ≥98.0%

NSC745885 是一种有效的抗肿瘤 (anti-tumor) 试剂，对多种癌细胞株有选择性毒性，但对正常细胞没有毒性。NSC745885 是一种有效的 EZH2 的下调因子通过蛋白酶体降解途径。NSC745885 为晚期膀胱癌和口腔鳞癌的研究提供了可能性。

NSC745885

NSC745885 Chemical Structure

CAS No. : 4219-52-7

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生物活性

NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers[1][2].

IC50 & Target[2]

EZH2

 

体外研究
(In Vitro)

NSC745885 (0.5-4 μM; 24, 48 or 72 hours) has a growth inhibitory or death-promoting effect on the SAS cells, it significantly decreases the densities of cultured cells when compared with untreated cells. The IC50 of NSC745885 is 0.85 μM after 72 hours’ treatment[1].
NSC745885 (0.5-4 μM; 24 hours) increases annexin V positive cells in a dose-dependent manner, and the differences appears as a dose-dependent manner[1].
NSC745885 (0.5-2 μM; 24 or 48 hours) decreases XIAP protein levels and increases protein levels both as a dose-dependent manner in SAS cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SAS cells is obtained from a poorly differentiated human squamous cell carcinoma
Concentration: 0.5 μM, 1 μM, 1.5 μM, 2 μM, 4 μM
Incubation Time: 24, 48, or 72 hours
Result: Decreases SAS cells growth as a time and dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: SAS cells is obtained from a poorly differentiated human squamous cell carcinoma
Concentration: 0.5 μM, 1 μM, 1.5 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Decreases SAS cells growth as a time and dose-dependent manner.

Western Blot Analysis[1]

Cell Line: SAS cells is obtained from a poorly differentiated human squamous cell carcinoma
Concentration: 0.5 μM, 1 μM, 1.5 μM, 2 μM
Incubation Time: 24 or 48 hours
Result: Increased cleaved caspase-3 expression and decreased XIAP expression.

体内研究
(In Vivo)

NSC745885 (intraperitoneal injection; 2 mg/kg; once daily; 10 days) treatment significantly reduces tumor size when compared with the vehicle control, and exhibits a higher safety than doxorubicin[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight-week-old NOD/SCID (NOD.CB17 Prkdcscid/J) mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection; 2 mg/kg; once daily; 10 days
Result: Inhibited engrafted tumors growth in vivo.

分子量

266.27

Formula

C14H6N2O2S
CAS 号

4219-52-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)

*NSC745885 is usually formulated as a suspension.
参考文献

  • [1]. Chen YW, et al.A novel compound NSC745885 exerts an anti-tumor effect on tongue cancer SAS cells in vitro and in vivo.PLoS One. 2014 Aug 15;9(8):e104703.

    [2]. Tang SH, et al. Pharmacologic down-regulation of EZH2 suppresses bladder cancer in vitro and in vivo.Oncotarget. 2014 Nov 15;5(21):10342-55.

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