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SC144
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SC144图片
CAS NO:895158-95-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
SC144 是首创的口服活性gp130 (IL6-beta)抑制剂。SC144 结合 gp130,诱导 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,进一步抑制下游靶基因的表达。SC144 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 诱导人卵巢癌细胞凋亡。
生物活性

SC144 is a first-in-class, orally activegp130 (IL6-beta)inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogatesStat3phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 inducesapoptosisin human ovariancancercells[1].

IC50& Target[1]

IL6-beta

 

体外研究
(In Vitro)

SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM)[1].
The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50=0.43 μM) and HEY (Cisplatin-resistant, IC50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer[1].
SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells[1].
SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner[1].
SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis[1].

Apoptosis Analysis[1]

Cell Line:OVCAR-8 and Caov-3 cells
Concentration:2 μM
Incubation Time:24 hours
Result:Significantly caused cell death in OVCAR-8 and Caov-3 cells.

Western Blot Analysis[1]

Cell Line:OVCAR-8, Caov-3 cells
Concentration:0.5-2 μM
Incubation Time:0-6 hours
Result:Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.
体内研究
(In Vivo)

SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts[1].
SC144 (100 mg/kg;p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group[1].

Animal Model:Athymic mice (human ovarian cancer xenograft)[1]
Dosage:10 mg/kg
Administration:I.p; daily for 58 days
Result:Significantly inhibited tumor growth by about 73%.
分子量

322.30

性状

Solid

Formula

C16H11FN6O

CAS 号

895158-95-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL(51.72 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.1027 mL15.5135 mL31.0270 mL
5 mM0.6205 mL3.1027 mL6.2054 mL
10 mM0.3103 mL1.5513 mL3.1027 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。