Name | TGFβRI-IN-2 |
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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]. |
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Related Catalog | |
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 |
Molecular Formula | C20H15ClFN5O2 |
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Molecular Weight | 411.82 |