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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
InChI
1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2
InChI 密鑰
IHLVSLOZUHKNMQ-UHFFFAOYSA-N
應用
LY2109761可用作I型和II型转变生长因子- β(TGFβ)受体的抑制剂,以降低HepG2细胞中SMAD2(母体抗生物皮肤生长因子同源物)的磷酸化。
生化/生理作用
LY2109761抑制增生性瘢痕中转变生长因子(TGF)-β1-诱导成纤维细胞增殖和胶原合成。因此,它用于治疗增生性瘢痕。
Ly2109761是一种高效、口服活性TGF-β受体(TGFβR)I型&II型双重抑制剂(针对TGFβRI/ALK5和TGFβRII自磷酸化分别为IC50 = 70和322 nM,及4μM ATP),仅在达到更高浓度(20 μM时抑制58-89%)时抑制Fyn/JNK3/Lck/MKK6/SAPK2α并对其他37种激酶(IC50 >20 μM)表现出微弱效力甚至没有效力。LY2109761可在培养物中抑制0.25 ng/mL TGFβ诱导的NIH/3T3(IC50 = 210 nM;TGFβ前2小时预处理24小时)并且抑制人MX1乳腺癌异种移植瘤在小鼠体内的生长(第37天∼80%;第7天到第20天75 mg/kg,每日口服两次)。在转移性胰腺癌小鼠模型中,与吉西他滨联合用药(25 mg/kg/天,经腹腔注射)时,LY2109761(50 mg/kg,每日口服两次)可显著降低转移性胰腺癌小鼠模型中的肿瘤负荷和自发性腹腔转移。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
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