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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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