NSC745885

生物活性靶点体外研究体内研究 NSC745885 试剂级价格

NSC745885

CAS号:4219-52-7
英文名:NSC745885
中文名:NSC745885
CBNumber:CB58054639
分子式:C14H6N2O2S
分子量:266.27
MOL File:4219-52-7.mol

NSC745885化学性质

沸点 :470.0±14.0 °C(Predicted)
密度 :1.574±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: < 1 mg/mL (insoluble or slightly soluble) *NSC745885 is usually formulated as a suspension.
形态 :Solid
酸度系数(pKa) :-1.90±0.20(Predicted)
颜色 :Light yellow to yellow

NSC745885性质、用途与生产工艺

生物活性 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。
靶点

EZH2

体外研究

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 IC ₅₀ of NSC745885 is 0.85 μM after 72 hours’ treatment.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.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.

Cell Viability Assay

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

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

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

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.

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