SC144

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SC144  纯度: 98.60%

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。

SC144

SC144 Chemical Structure

CAS No. : 895158-95-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥990 In-stock
5 mg ￥900 In-stock
10 mg ￥1300 In-stock
25 mg ￥2400 In-stock
50 mg ￥4080 In-stock
100 mg ￥6950 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SC144 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Orally Active Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library

生物活性

SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells[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].

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.

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].

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: 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

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1027 mL 15.5135 mL 31.0270 mL
5 mM 0.6205 mL 3.1027 mL 6.2054 mL
10 mM 0.3103 mL 1.5513 mL 3.1027 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Xu S, et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务