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917497-70-2

中文名稱 CS-2091
英文名稱 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
CAS 917497-70-2
分子式 C17H12ClFN6O3
分子量 402.767
MOL 文件 917497-70-2.mol
更新日期 2024/07/01 17:51:33
917497-70-2 結(jié)構(gòu)式 917497-70-2 結(jié)構(gòu)式

基本信息

中文別名
N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼鹽酸鹽
英文別名
CS-2091
SC144 HCl
SC144 hydrochloride
N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide
N’-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide Hydrochloride
2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl) 2-pyrazinecarboxylic acid hydrazide hydrochloride
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

熔點282 °C (decomp)(Solv: methanol (67-56-1))
儲存條件-20°C
溶解度DMSO:可溶5mg/mL,澄清(加熱)
形態(tài)粉末
顏色白色至淺棕色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
危險品標志Xi
危險類別碼36/37/38
安全說明26-36/39
WGK Germany3
CS-2091價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-15614ACS-2091
SC144 hydrochloride
917497-70-25mg900元
2024/11/08HY-15614ACS-2091
SC144 hydrochloride
917497-70-210mM * 1mLin DMSO990元
2024/11/08HY-15614ACS-2091
SC144 hydrochloride
917497-70-210mg1300元

常見問題列表

生物活性
SC144 hydrochloride 是首創(chuàng)的口服活性 gp130 (IL6-beta) 抑制劑。SC144 hydrochloride 結(jié)合 gp130,誘導 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,進一步抑制下游靶基因的表達。SC144 hydrochloride 對 gp130 配體觸發(fā)的信號轉(zhuǎn)導有明顯的抑制作用。SC144 hydrochloride 誘導人卵巢癌細胞凋亡。
靶點

IL6-beta

體外研究

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.
體內(nèi)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%.
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