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Galunisertib {[allProObj[0].p_purity_real_show]}

货号：A150887 同义名： LY2157299

Galunisertib 是一种高效 TGF-βRI 激酶抑制剂（IC50 = 56 nM），在癌症细胞模型中常用于阻断 TGF-β 信号通路并评估其对细胞迁移与侵袭的影响。

Galunisertib 化学结构 CAS号：700874-72-2
Galunisertib 化学结构
CAS号：700874-72-2
Galunisertib 3D分子结构
CAS号：700874-72-2
Galunisertib 化学结构 CAS号：700874-72-2
Galunisertib 3D分子结构 CAS号：700874-72-2
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Galunisertib 纯度/质量文件 产品仅供科研

货号：A150887 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

 		++++

ALK2, IC50: 1.3 nM

 		+

ALK3, IC50: 85.8 nM

 		+

ALK4, IC50: 2133 nM

 		+

ALK5, IC50: 9276 nM

 		99%+
ML347 ++

ALK1, IC50: 46 nM

 		++

ALK2, IC50: 32 nM

 		98%
K02288 ++++

ALK1, IC50: 1.8 nM

 		++++

ALK2, IC50: 1.1 nM

 		++

ALK3, IC50: 34.4 nM

 		+++

ALK6, IC50: 6.4 nM

 		99%+
LDN-193189 2HCl ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%
LDN-214117 ++

ALK2, IC50: 24 nM

 		98%
DMH-1 +

ALK2, IC50: 107.9 nM

 		99%+
SB-505124 +

ALK4, IC50: 129 nM

 		++

ALK5, IC50: 47 nM

 		99%+
Vactosertib +++

ALK4, IC50: 13 nM

 		+++

ALK5, IC50: 11 nM

 		99%+
Alantolactone ✔ 98%
(E/Z)-SIS3 free base ✔ 97%
Pirfenidone ✔ 98%
Hesperetin ✔ 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

 		98%
GW788388 +++

ALK5, IC50: 18 nM

 		98%
LY364947 ++

TGFβRI, IC50: 59 nM

 		+

TGFβRII, IC50: 0.4 μM

 		98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

 		99%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

 		99%+
LY2109761 ++

TβRI, Ki: 38 nM

 		+

TβRII, Ki: 300 nM

 		99%+
Galunisertib ++

TβRI, IC50: 56 nM

 		98%
SB 431542 +

ALK5, IC50: 94 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Galunisertib 生物活性

靶点

  • TGFβRI/ALK5

    TβRI, IC50:56 nM
描述 The TGF-β pathway regulates a wide variety of cellular processes in many different cell types and biological contexts. There are three identified TGF receptor ligands, TGF-β1, 2, and 3. Activated TGF-β ligands can interact with TGF-β type II receptors (TβRII), then recruit and phosphorylate the TGF-β type I receptors (also called as TβRI or ALK5). In turn, activated TβRI phosphorylates SMAD2 and SMAD3 at C-terminal serine residues. Following that, phosphorylated SMAD and SMAD3 assemble into heterodimeric and trimeric complexes with SMAD4. Then the trimeric complex translocate into the nucleus and regulate the expression of TGF-β target genes[1]. LY2157299 (Galunisertib) is a selective TGF-β1 Type I receptor inhibitor with IC50 values of 0.17, 0.21 and 0.08 nM for TGF-βRI, TGF-βRII and ALK4 (measure by kinase assays)[2] Pre-treatment with 0.5 μM LY2157299 for 1h can abolish or reduce SMAD2 phosphorylation induced by TGF-β-activated TBRI in HS-5 and K562 cells. After 14 days of oral administration of LY-2157299, 100 mg/kg, daily, anemia in a model of bone marrow failure was improved. LY-2157299 can result in a significant increase in erythroid and myeloid colony numbers in all patients, which pointed to a high therapeutic potential of TβRI inhibition by LY2157299 in low-grade MDS[3]. Orally administered with LY2157299 (75 mg/kg, bid) significantly suppress growth of transplanted tumors in B16 cells xenograft mice[4]. Up to now, a phase 3 study of LY2157299 treatment for Myelodysplastic Syndromes, as well as phase 2 studies of LY2157299 treatment for glioma has been completed. The phase 2 studies of LY2157299 treatment for solid tumor, non-small cell lung cancer recurrent and hepatocellular carcinoma recurrent are recruiting (see https://www.clinicaltrials.gov/).
作用机制 LY2157299 binds to the ATP-binding site of TGFβRI.

Galunisertib 细胞实验

Cell Line
Concentration Treated Time Description References
human naïve CD4+ T cells 10 µg/ml 5 days Galunisertib potently suppressed the differentiation of PD-1+CXCR5+ cells induced by Activin A Nat Immunol. 2016 Aug;17(8):976-84.
HLE cells 10 µM 48 h Galunisertib significantly reduced the expression of CD44 and THY1 in HLE and HLF cells, indicating that Galunisertib modulates the stemness phenotype of HCC cells by inhibiting the TGF-β signaling pathway. Cell Death Dis. 2018 Mar 7;9(3):373.
AGS cells 5 µM 8 h Inhibition of TGF-β1 signaling pathway, reversal of EMT activation Cell Mol Life Sci. 2024 Nov 15;81(1):453.
SGC-7901 cells 5 µM 8 h Inhibition of TGF-β1 signaling pathway, reversal of EMT activation Cell Mol Life Sci. 2024 Nov 15;81(1):453.
HLF cells 10 µM 48 h Galunisertib significantly reduced the expression of CD44 and THY1 in HLE and HLF cells, indicating that Galunisertib modulates the stemness phenotype of HCC cells by inhibiting the TGF-β signaling pathway. Cell Death Dis. 2018 Mar 7;9(3):373.
HLF cells 10 μM 2 h and 48 h To study the effect of Galunisertib on TGF-β1-induced gene expression, results showed that Galunisertib inhibited TGF-β1-induced gene upregulation. Cell Death Dis. 2017 Feb 23;8(2):e2634.
HepG2 cells 10 μM 2 h and 24 h To study the effect of Galunisertib on TGF-β1-induced gene expression in HepG2 cells, results showed that Galunisertib had different effects on gene expression at different time points. Cell Death Dis. 2017 Feb 23;8(2):e2634.
HLE cells 10 μM 2 h and 24 h To study the effect of Galunisertib on TGF-β1-induced gene expression in HLE cells, results showed that Galunisertib had different effects on gene expression at different time points. Cell Death Dis. 2017 Feb 23;8(2):e2634.
Panc1 10μM 48 h To evaluate the effect of chemotherapeutic agents on tumor cell immunogenicity. Cancer Res. 2020 Aug 1;80(15):3101-3115.
hPSC 10μM 48 h To evaluate the effect of Galunisertib on immunomodulatory proteins in hPSC cells, results showed that Galunisertib significantly inhibited the induction of immunomodulatory proteins by Panc1-GR conditioned media Cancer Res. 2020 Aug 1;80(15):3101-3115.
HepG2 cells 10 µM 48 h Galunisertib significantly inhibited the TGFβ1-induced phosphorylation of Smad2 and Smad3, indicating that the 3D liver scaffolds can be used as a drug screening platform. Cells. 2019 Dec 28;9(1):83.

Galunisertib 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Subcutaneous tumor model Intraperitoneal injection 300 µg/mouse Every 5 days for 3 weeks Galunisertib treatment significantly reduced the volume and weight of subcutaneous tumors Cell Mol Life Sci. 2024 Nov 15;81(1):453.
Mice SMAD4-deficient colorectal cancer model Oral 75 mg/kg Once daily for 7 days Galunisertib inhibited the metastasis rate of SMAD4-deficient CRC cells and significantly reduced the proportion of intratumoral G-MDSCs. Acta Pharm Sin B. 2024 Aug;14(8):3711-3729
Nude mice Subcutaneous xenograft model Oral 800 mg/kg Once daily for an appropriate duration Galunisertib treatment rescued the increased tumor growth and lung metastasis caused by HOOK1 knockdown, thereby prolonging the survival of tumor-bearing nude mice Adv Sci (Weinh). 2023 Jun;10(17):e2206955
Mice KC and KCT mouse models Intraperitoneal injection 75mg/kg Twice weekly for four months To evaluate the effect of combined Galunisertib and anti-PD-1 therapy on pancreatic cancer, results showed that in the setting of TGFβ signaling deficiency, the combination therapy significantly enhanced CD8+ T-cell response and reduced tumor burden Cancer Res. 2020 Aug 1;80(15):3101-3115.

Galunisertib 动物研究

Dose Mice[6] (p.o.): 150 mg/kg, 1.5 mg/kg (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Nude mice[7]
Dose 75 mg/kg
Administration p.o.
VT/F 2.02 ± 0.11 L
V/F 0.64 ± 0.58 L
CLD/F 1.05 ± 0.33 L/h
Cl/F 0.57 ± 0.08 L/h

Galunisertib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03206177 Carcinosarcoma, Ovarian Phase 1 Recruiting June 1, 2022 United States, Oklahoma ... 展开 >> University of Oklahoma Health Sciences Center Recruiting Oklahoma City, Oklahoma, United States, 73104 Contact: Kathleen Moore, MD 收起 <<
NCT01373164 Neoplasms Neo... 展开 >>plasm Metastasis Pancreatic Cancer 收起 << Phase 1 Phase 2 Completed - United States, Florida ... 展开 >> Florida Hospital Tampa HPG and Foregut Surgery Tampa, Florida, United States, 33613 United States, Illinois Ingalls Memorial Hospital Harvey, Illinois, United States, 60426 United States, Washington Seattle Cancer Care Alliance Seattle, Washington, United States, 98109 Belgium For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Brussel, Belgium, 1000 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Liège, Belgium, 4000 France For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Besancon, France, 25030 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Clermont-Ferrand, France, 63003 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Marseille, France, 13273 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Montbéliard, France, 25250 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Paris, France, 75674 Germany For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Frankfurt, Germany, 60596 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Friedrichshafen, Germany, 88045 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Leipzig, Germany, 04103 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Marburg, Germany, 35043 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Munich, Germany, 81925 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Mönchengladbach, Germany, 41063 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Reutlingen, Germany, 72764 Italy For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Bergamo, Italy, 24128 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Bologna, Italy, 40138 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Verona, Italy, 37134 Spain For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Barcelona, Spain, 08035 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Madrid, Spain, 28033 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Pozuelo De Alarcon, Spain, 28223 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Sevilla, Spain, 41013 收起 <<
NCT01373164 - Completed - -

Galunisertib 参考文献

[1]Colak S, Ten Dijke P, et al. Targeting TGF-β Signaling in Cancer. Trends Cancer. 2017 Jan;3(1):56-71.

[2]Herbertz S, Sawyer JS, et al. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. Drug Des Devel Ther. 2015 Aug 10;9:4479-99.

[3]Zhou L, McMahon C, et al. Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase. Cancer Res. 2011 Feb 1;71(3):955-63.

[4]Yoon JH, Jung SM, et al. Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes. EMBO Mol Med. 2013 Nov;5(11):1720-39.

[5]Yingling JM, McMillen WT, et al. Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor. Oncotarget. 2017 Dec 31;9(6):6659-6677.

[6]Faivre S, Santoro A, et al. Novel transforming growth factor beta receptor I kinase inhibitor galunisertib (LY2157299) in advanced hepatocellular carcinoma. Liver Int. 2019 Aug;39(8):1468-1477.

[7]Bueno L, de Alwis DP, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50. Epub 2007 Nov 26.

Galunisertib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL

Galunisertib 技术信息

CAS号700874-72-2
分子式C22H19N5O
分子量 369.42
SMILES Code O=C(C1=CC=C2N=CC=C(C3=C(CCC4)N4N=C3C5=NC(C)=CC=C5)C2=C1)N
MDL No. MFCD12923319
别名 LY2157299
运输蓝冰
InChI Key IVRXNBXKWIJUQB-UHFFFAOYSA-N
Pubchem ID 10090485
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 105 mg/mL(284.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四

Tags: Galunisertib | LY2157299 | TGF-beta/Smad | AmBeed-信号通路专用抑制剂 | Galunisertib 纯度/质量文件 | Galunisertib 亚型比较 | Galunisertib 生物活性 | Galunisertib 动物研究 | Galunisertib 临床数据 | Galunisertib 参考文献 | Galunisertib 实验方案 | Galunisertib 技术信息

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