895158-95-9

中文名称吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼

英文名称 SC 144

CAS 895158-95-9

分子式 C16H11FN6O

分子量 322.3

MOL 文件 895158-95-9.mol

更新日期 2024/04/15 22:10:26

895158-95-9 结构式

基本信息物理化学性质安全数据常见问题列表图谱信息

基本信息

中文别名

GP130抑制剂(SC144)
2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪羧酸酰肼
吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼

英文别名

SC144
SC 144
SC-144
CS-805
SC 144
SC144
SC144
SC-144
SC 144
2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide
N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazide
Pyrazinecarboxylic acid 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide
2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide

所属类别

生物化工：激动剂抑制剂

物理化学性质

密度1.53±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度insoluble in EtOH; insoluble in H2O; ≥16.1 mg/mL in DMSO

酸度系数(pKa)8.87±0.43(Predicted)

形态固体

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H315-H319-H335

防范说明P261-P280-P301+P312-P302+P352-P305+P351+P338

常见问题列表

简介

SC144是一种口服活性小分子gp130抑制剂。

生物活性

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。

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:	10 mg/kg
Administration:	I.p; daily for 58 days
Result:	Significantly inhibited tumor growth by about 73%.

图谱信息

吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼(895158-95-9)核磁图(¹HNMR)