| Chemical Properties | Back Directory | [Boiling point ]
664.2±65.0 °C(Predicted) | [density ]
1.450±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
15.82±0.40(Predicted) | [color ]
White to off-white | [InChI]
1S/C20H15ClFN5O2/c1-11-8-25-15(13-6-12(21)2-3-14(13)22)7-17(11)27-16-4-5-24-9-18(16)26(20(27)29)10-19(23)28/h2-9H,10H2,1H3,(H2,23,28) | [InChIKey]
LVEUPFUJRKZPEN-UHFFFAOYSA-N | [SMILES]
Fc1c(cc(cc1)Cl)c2ncc(c(c2)[n]3c4c([n]([c]3=O)CC(=O)N)cncc4)C |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
SGC Frankfurt Pharma donated probe. TP-008 is a cell penetrantpotent and selective ALK4/5 ((activin-like kinase 4/5) dual inhibitor th at potently inhibits SMAD2/3 phosphorylation in C2C12 cells. TP-008 exhibits significant cardiac toxicity in mice. It is compound 18 in BMCL 2016 paper. | [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: | 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. DOI:10.1016/j.bmcl.2016.07.030 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|