LY 3200882

SKU: orb1225818

Description

LY 3200882 (LY3200882) is a novel potent, highly selective, ATP competitive TGF-β receptor type 1 (TGFβRI, ALK5) inhibitor; potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors; LY 3200882 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.Solid Tumors Phase 1 Clinical(In Vitro):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.(In Vivo):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).

Key Properties

• CAS Number: 1898283-02-7
• MW: 435.528
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₉N₅O₃
• SMILES: CC(O)(C)C1=NC=CC(NC2=NC=CC(OC3=CN(C4CC4)N=C3C5CCOCC5)=C2)=C1
• Target: TGFBR
• Solubility: DMSO: 85 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LY3200882

Quick Database Links

Gene Symbol

TGFBR