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198481-32-2

中文名稱 巴多昔芬
英文名稱 Bazedoxifene
CAS 198481-32-2
分子式 C30H34N2O3
分子量 470.6
MOL 文件 198481-32-2.mol
更新日期 2024/10/09 11:06:38
198481-32-2 結(jié)構(gòu)式 198481-32-2 結(jié)構(gòu)式

基本信息

中文別名
巴多昔芬
巴多兮芬
巴佐昔芬雜質(zhì)
巴多昔芬中間體
1-(4-(2-(氮雜環(huán)庚烷-1-基)乙氧基)芐基)-2-(4-羥基苯基)-3-甲基-1H-吲哚-5-醇
1-[[4-[2-(氮雜環(huán)庚烷-1-基)乙氧基]苯基]甲基]-2-(4-羥基苯基)-3-甲基-吲哚-5-醇
英文別名
Tse-424
CS-1993
Batoxifene
Bazedoxifen
Bazedoxifene
Bazedoxifeno
Unii-Q16tt9C5bk
BAZEDOXIFENE BASE
Bazedoxifene [inn]
Bazedoxifene free base
所屬類別
生物化工:抑制劑

物理化學(xué)性質(zhì)

熔點98-102°
沸點694.4±55.0 °C(Predicted)
密度1.19
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度可溶于氯仿(少許)、DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)10.12±0.15(Predicted)
形態(tài)固體
顏色白色至深米色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS08
警示詞危險
危險性描述H360

常見問題列表

生物活性
Bazedoxifene (TSE-424) 是一種有口服活性的,能透過血腦屏障的,非甾體、選擇性的雌激素受體調(diào)節(jié)劑 (SERM),對 ERα 和 ERβ 作用的 IC50 值分別為 26 nM 和 99 nM,可用于骨質(zhì)疏松癥的研究。Bazedoxifene 也是一種 IL-6/GP130 蛋白相互作用抑制劑,可用于胰腺癌的研究。
靶點

IC50: 26 nM (ERα), 99 nM (ERβ)

體外研究

Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.
Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.
Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.
Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.
Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6.
Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130.

Western Blot Analysis

Cell Line: AsPC-1 cells
Concentration: 10 μM, 20 μM
Incubation Time: 2 hours
Result: Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation.

Apoptosis Analysis

Cell Line: Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells
Concentration: 10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC)
Incubation Time: Overnight
Result: Induced apoptosis.
體內(nèi)研究

Bazedoxifene (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo.

Animal Model: 6-week-old female athymic nude mice
Dosage: 5 mg/kg
Administration: Oral gavage, daily, for 18 days
Result: Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.
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