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LY3200882
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY3200882图片
CAS NO:1898283-02-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 435.53
Formula C24H29N5O3
CAS No. 1898283-02-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 130 mg/mL
Water: N/A
Ethanol: N/A
Chemical Name2-(4-((4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)oxy)pyridin-2-yl)amino)pyridin-2-yl)propan-2-ol
SynonymsLY 3200882; LY3200882; LY-3200882;
实验参考方法
In Vitro

In vitro activity: LY3200882 is a next generation, ATP competitive, potent, highly selective small molecule inhibitor of TGF-β receptor type 1 (TGFβRI). It inhibits the serine-threonine kinase domain of TGFβRI. LY3200882 inhibits various pro-tumorigenic activities. LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. In preclinical tumor models, LY3200882 showed potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment.


Kinase Assay: In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naive T cell activity and restore proliferation. Therefore, LY3200882 shows promising activity as an immune modulatory agent. In addition, LY3200882 has shown anti-metastatic activity in vitro in migration assays as well as in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer).


Cell Assay: LY3200882 is a next generation, ATP competitive, potent, highly selective small molecule inhibitor of TGF-β receptor type 1 (TGFβRI). It inhibits the serine-threonine kinase domain of TGFβRI. LY3200882 inhibits various pro-tumorigenic activities.

In Vivo LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. In preclinical tumor models, LY3200882 showed potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment. Durable tumor regressions in the orthotopic 4T1-LP model were observed and rechallenge of congenic tumors resulted in complete rejection in all mice.
Animal model Mice with orthotopic 4T1-LP model of triple negative breast cancer
Formulation & Dosage
References AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955.