| 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 |
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| Target |
IC50: ALK 5[1]
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| 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].
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| 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.
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| 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.
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