TGFβRI-IN-2

Names

[ CAS No. ]:
1976038-41-1

[ Name ]:
TGFβRI-IN-2

Biological Activity

[Description]:

TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose[1].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK

Research Areas >> Inflammation/Immunology

[Target]

IC50: ALK 5[1]

[In Vitro]

TGFβRI-IN-2 (compound 18) at 1 μM shows a 31% inhibition of MAP3K2 (MEKK2) with an IC50 value of 2.2 μM[1].

[In Vivo]

TGFβRI-IN-2 (oral administation; 50, 150 and 500 mg/kg; 5 days) induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves[1]. Animal Model: Rats[1] Dosage: 50, 150 and 500 mg/kg Administration: Oral administation; 50, 150 and 500 mg/kg; 5 days Result: Induced cardiovalvulopathy in both the medium and high dose animal groups.

[References]

[1]. Wang H, et al. Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.Bioorg Med Chem Lett. 2016 Sep 1;26(17):4334-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₁₅ClFN₅O₂

[ Molecular Weight ]:
411.82

TGFβRI-IN-2

Names

Biological Activity

Chemical & Physical Properties

Related Compounds