Galunisertib (LY2157299)

For research use only. Not for use in humans.

目录号:S2230

Galunisertib (LY2157299) Chemical Structure

CAS No. 700874-72-2

Galunisertib (LY2157299)是有效的TGFβ receptor I (TβRI)抑制剂,无细胞试验中IC50为56 nM。Phase 2/3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2228.23 现货
RMB 1377.29 现货
RMB 2191.21 现货
RMB 6303.16 现货
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客户使用Selleck生产的Galunisertib (LY2157299)发表文献75篇:

产品安全说明书

TGF-beta/Smad抑制剂选择性比较

生物活性

产品描述 Galunisertib (LY2157299)是有效的TGFβ receptor I (TβRI)抑制剂,无细胞试验中IC50为56 nM。Phase 2/3。
靶点
TβRI [1]
(Cell-free assay)
56 nM
体外研究

LY2157299有效地抑制了TGFβ受体信号。LY2157299抑制了HUVEC细胞中TGFβ诱导的Smad2的磷酸化。在HUVEC细胞中,LY2157299也呈剂量依赖性增强了VEGF或bFGF在血管内皮细胞诱导的细胞增殖作用。LY2157299也促进VEGF诱导的HUVEC细胞迁移。在体外的VEGF刺激的帘线形成测定中,LY2157299可加强血管生成。[2] 在初级造血干细胞中,LY2157299以剂量依赖的方式抑制TGF-β介导的SMAD2活化和造血抑制。LY2157199刺激原发性MDS骨髓的造血功能。[3] 在人类胶质母细胞瘤(GBM)细胞中,LY2157299通过TGFβ受体复合物处抑制信号通路活性,减少活性磷酸化SMAD的水平。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Panc-1 MlzSSpVv[3Srb36gRZN{[Xl? MnjONVAh|ryP NVLWXnd4PDhiaB?= MmnrSG1UVw>? MVrzeIlufWyjdHXzJJRp\SClZXzsJIlvfmG|aX;uJIlvfG9idHjlJINwdGyjZ3XuJIdmdCCjbnSgeIhmKE2jdILp[4VtNWOxYYTl[EBkd2yuYXflckBo\Wx? MUiyOFc5ODh{MR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Periostin / Fibronectin / Snail / Twist / pSmad2 / pERK / pAkt / pFAK; 

PubMed: 29774119     


U-87 MG cells were serum-starved for 24 h, then incubated in serum-free medium containing (or lacking) 10 μM Galunisertib (LY2157299) and 10 ng/mL of TGF-β for 48 h. Cells were lysed and expression levels of EMT markers periostin, fibronectin, Snail and twist, or the phosphorylation status of Smad2, Erk, Akt and Fak proteins were monitored by immunoblotting.

TGF-βR1 / p-ERK; 

PubMed: 30881035     


Western blot was performed to analyze the expression level of TGF-βR1, p-smad2 and p-ERK1/2. VECTOR, cells transduced with VECTOR lentivirus; VECTOR+ LY2157299, cells transduced with VECTOR lentivirus and treated with LY2157299; USP4, cells transduced with USP4 lentivirus; USP4+ LY2157299, cells transduced with USP4 lentivirus and treated with LY2157299.

29774119 30881035
Growth inhibition assay
Cell viability; 

PubMed: 28873435     


Primary cell cultures were treated with LY2157299. MTS was performed at 72 hrs. TGF-ΒR1 inhibition by LY2157299 did not influence cell viability in any type of primary cell culture. 

28873435
Immunofluorescence
E-cadherin; 

PubMed: 29467918     


KPC-M09 cells were treated with control, TGFβ or TGFβ plus galunisertib (2 μM or 10 μM). Bright field images are shown in the top panel and were imaged at 20X. The bottom panel shows fluorescent IHC using anti-E-cadherin (red) as well as DAPI (blue) as a counter stain. Cells were imaged at 40X.

29467918
体内研究 虽然抗肿瘤活性已经在一些临床前模型中观察到了,但在4T1,Colo205,或A549异种移植模型中,LY2157299并没有显著抑制体内血管生成的作用。[2] 在TGF-β过度表达的转基因骨髓造血功能衰竭小鼠模型中,LY2157299可改善贫血。[3] 在Calu6和MX1异种移植物小鼠中,LY2157299(75 mg/kg/day,口服)给药显示显著抗肿瘤活性。[5] 在体内基质胶栓法检测中,LY2157299诱导血管生成并增强VEGF和碱性成纤维细胞生长因子诱导的血管生成,而在基底膜中添加alpha5-整合素中和抗体抑制这种增强应答。[6]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[5]
- 合并
  • Animal Models: 裸鼠皮下植入Calu6或MX1细胞
  • Dosages: 75 mg/kg/day
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 74 mg/mL (200.31 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1%CMC-Na
30mg/mlmg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 369.42
化学式

C22H19N5O

CAS号 700874-72-2
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04031872 Not yet recruiting Drug: LY3200882 Colorectal Cancer Metastatic The Netherlands Cancer Institute|Vall d''Hebron Institute of Oncology|Agendia|European Organisation for Research and Treatment of Cancer - EORTC|Azienda Ospedaliera Niguarda Cà Granda|Fundación para la Investigación del Hospital Clínico de Valencia|University of Campania Luigi Vanvitelli|University of Turin Italy|Eli Lilly and Company|Catalan Institute of Health|Universitaire Ziekenhuizen Leuven February 2020 Phase 1|Phase 2
NCT03470350 Withdrawn Drug: Galunisertib Colorectal Cancer Metastatic The Netherlands Cancer Institute|Vall d''Hebron Institute of Oncology|Agendia|European Organisation for Research and Treatment of Cancer - EORTC|Azienda Ospedaliera Niguarda Cà Granda|Fundación para la Investigación del Hospital Clínico de Valencia|University of Campania Luigi Vanvitelli|University of Turin Italy|Eli Lilly and Company|Catalan Institute of Health|Universitaire Ziekenhuizen Leuven August 24 2018 Phase 1|Phase 2
NCT02734160 Completed Drug: Galunisertib|Drug: Durvalumab Metastatic Pancreatic Cancer Eli Lilly and Company|AstraZeneca June 15 2016 Phase 1
NCT02452008 Recruiting Drug: Enzalutamide|Drug: LY2157299 Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Eli Lilly and Company May 3 2016 Phase 2
NCT02752919 Completed Drug: Galunisertib Healthy Eli Lilly and Company April 2016 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID