产品
编 号：F237373
分子式：C24H29N5O3
分子量：435.52
分子式：C24H29N5O3
分子量：435.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
436
In-stock
5mg
960
In-stock
10mg
1520
In-stock
50mg
5200
In-stock
结构图
CAS No: 1898283-02-7
产品详情
生物活性：
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
体内研究：
LY3200882 (60 mg/kg; oral gavage; twice a day; for 21 days; BALB/C female mice) treatment significantly delays tumor growth in CT26 model.LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion.LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer).Animal Model:BALB/C female mice (5-8-week-old) injected with CT26 cells
Dosage:60 mg/kg
Administration:Oral gavage; twice a day; for 21 days
Result:A statistically significant tumor growth delay in CT26 model was observed.
体外研究：
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells in a dose dependent fashion. LY3200882 shows 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.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.LY3200882 inhibits NIH3T3 cell viability with an IC50 of 82.9 nM.
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
体内研究：
LY3200882 (60 mg/kg; oral gavage; twice a day; for 21 days; BALB/C female mice) treatment significantly delays tumor growth in CT26 model.LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion.LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer).Animal Model:BALB/C female mice (5-8-week-old) injected with CT26 cells
Dosage:60 mg/kg
Administration:Oral gavage; twice a day; for 21 days
Result:A statistically significant tumor growth delay in CT26 model was observed.
体外研究：
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells in a dose dependent fashion. LY3200882 shows 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.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.LY3200882 inhibits NIH3T3 cell viability with an IC50 of 82.9 nM.
产品资料
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