SC144 hydrochloride|917497-70-2|-陌孚医药/Medlife

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SC144 hydrochloride

目录号: PL13368 纯度: ≥99%

CAS No. :917497-70-2

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中文名称	SC144 hydrochloride
英文名称	SC144 hydrochloride
英文别名	SC 144 hydrochloride;2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride;SC-144 hydrochloride;SC144 (hydrochloride);SC144 hydrochloride;AOB4427;BCP19383;N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide hydrochloride;SY263534;2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl) 2-pyrazinecarboxylic acid hydrazide hydrochloride;N'-(7-fluoropyrrolo[1,2-a]quinoxa
Cas No.	917497-70-2
分子式	C₁₆H₁₂ClFN₆O
分子量	358.76
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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，进一步抑制下游靶基因的表达。SC144 hydrochloride 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 hydrochloride 诱导人卵巢癌细胞凋亡。
生物活性	SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
性状	Solid
IC50 & Target[1][2]	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). 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. SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells. 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.
体内研究(In Vivo)	SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.

溶解度数据	In Vitro: DMSO : 10 mg/mL (27.87 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液

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