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SC144 hydrochloride

产品编号 T41260 CAS 917497-70-2

SC144 hydrochloride 是首创的口服活性gp130 (IL6-beta)抑制剂。SC144 hydrochloride 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，进而抑制下游靶基因的表达。SC144 hydrochloride 对 gp130 配体触发的信号转导显示有效的抑制作用。SC144 hydrochloride 诱导人卵巢癌细胞凋亡。

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SC144 hydrochloride, CAS 917497-70-2

规格	价格/CNY	货期
2 mg	￥ 457	5日内发货
5 mg	￥ 747	5日内发货
10 mg	￥ 1,280	5日内发货
1 mL * 10 mM (in DMSO)	￥ 822	5日内发货

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SC144 hydrochloride 的其他形式现货产品:

SC144

其他形式的 SC144 hydrochloride:

SC144
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生物活性

化学信息

存储 & 溶解度

产品描述	SC144 hydrochloride, a first-in-class, orally active, small-molecule gp130 (IL6-beta) inhibitor, demonstrates potent inhibition of gp130 ligand-triggered signaling. By binding to gp130, it initiates gp130 phosphorylation (S782) and deglycosylation, impedes Stat3 phosphorylation and nuclear translocation, and suppresses the expression of downstream target genes. Furthermore, SC144 hydrochloride effectively induces apoptosis in human ovarian cancer cells [1].
体外活性	SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC 50 s in a submicromolar range (IC 50 =OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM) [1]. The potency of SC144 against NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC 50 =0.43 μM) and HEY (Cisplatin-resistant, IC 50 =0.88 μM) demonstrates 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.
体内活性	SC144 (10 mg/kg; i.p.; daily for 58 days) delays 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: I.p; daily for 58 days Administration: 10 mg/kg Result: Significantly inhibited tumor growth by about 73%.

分子量	358.76
分子式	C16H12ClFN6O
CAS No.	917497-70-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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对于不同动物的给药剂量换算，您也可以参考 更多...

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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