SML2051
LY2109761
≥98% (HPLC)
别名:
4-[5,6-二氢-2-（2-吡啶）-4H-吡咯[1,2-b]吡唑-3-基]-7-[2-（4-吗啉）乙氧基]-喹啉, LY-2109761
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关于此项目
经验公式（希尔记法）:
C26H27N5O2
化学文摘社编号:
分子量:
441.52
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
产品名称
LY2109761, ≥98% (HPLC)
SMILES string
[n]21nc(c(c2CCC1)c4c5c(ncc4)cc(cc5)OCCN6CCOCC6)c3ncccc3
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 key
IHLVSLOZUHKNMQ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
相关类别
Application
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。
Biochem/physiol Actions
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。
口服活性、强效和选择性TGFβRI/II双重抑制剂，在培养物中和体内具有抗癌功效。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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