| Bioactivity | TP-008 is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 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]. |
| Target | IC50: ALK 5 |
| Invitro | TP-008 at 1 μM shows a 31% inhibition of MAP3K2 (MEKK2) with an IC50 value of 2.2 μM[1]. |
| In Vivo | TP-008 (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: |
| Name | TP-008 |
| CAS | 1976038-41-1 |
| Formula | C20H15ClFN5O2 |
| Molar Mass | 411.82 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
TP-008
CAS: 1976038-41-1 F: C20H15ClFN5O2 W: 411.82
TP-008 is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.
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