LY 3200882

CAS No. 1898283-02-7

LY 3200882( LY3200882 )

Catalog No. M12981 CAS No. 1898283-02-7

LY 3200882 (LY3200882) is a novel potent, highly selective, ATP competitive TGF-β receptor type 1 (TGFβRI, ALK5) inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 58 In Stock
5MG 96 In Stock
10MG 152 In Stock
25MG 285 In Stock
50MG 462 In Stock
100MG 669 In Stock
500MG 1395 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    LY 3200882
  • Note
    Research use only, not for human use.
  • Brief Description
    LY 3200882 (LY3200882) is a novel potent, highly selective, ATP competitive TGF-β receptor type 1 (TGFβRI, ALK5) inhibitor.
  • 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).
  • 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). 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.
  • Synonyms
    LY3200882
  • Pathway
    TGF-beta/Smad
  • Target
    TGFBR
  • Recptor
    TGF-beta/Smad
  • Research Area
    Cancer
  • Indication
    Solid Tumors

Chemical Information

  • CAS Number
    1898283-02-7
  • Formula Weight
    435.528
  • Molecular Formula
    C24H29N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 85 mg/mL ( < 1 mg/ml refers to the product slightly soluble or insoluble )
  • SMILES
    CC(O)(C)C1=NC=CC(NC2=NC=CC(OC3=CN(C4CC4)N=C3C5CCOCC5)=C2)=C1
  • Chemical Name
    4-[[4-[[1-Cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]oxy]-2-pyridinyl]amino]-α,α-dimethyl-2-pyridinemethanol

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR. DOI: 10.1158/1538-7445.
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