CS-2091

生物活性靶点体外研究体内研究 CS-2091 试剂级价格

CS-2091

CAS号:917497-70-2
英文名:2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
中文名:CS-2091
CBNumber:CB72750597
分子式:C17H12ClFN6O3
分子量:402.7669832
MOL File:917497-70-2.mol

CS-2091化学性质

熔点 :282 °C (decomp)(Solv: methanol (67-56-1))
储存条件 :-20°C
溶解度 :DMSO: soluble5mg/mL, clear (warmed)
形态 :powder
颜色 :white to light brown

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26-36/39
WGK Germany :3

CS-2091性质、用途与生产工艺

生物活性 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。
靶点

IL6-beta

体外研究

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).
The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC ₅₀ =0.43 μM) and HEY (Cisplatin-resistant, IC ₅₀ =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.
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.

Apoptosis Analysis

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

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

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.

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