| Identification | Back Directory | [Name]
1H-Pyrrolo[2,3-b]pyridine-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3Z)- | [CAS]
1448874-96-1 | [Synonyms]
ansornitinib
1H-Pyrrolo[2,3-b]pyridine-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3Z)- | [Molecular Formula]
C30H32N6O4 | [MOL File]
1448874-96-1.mol | [Molecular Weight]
540.62 |
| Chemical Properties | Back Directory | [Boiling point ]
767.3±60.0 °C(Predicted) | [density ]
1.307±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
9.47±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases[1]. | [in vivo]
Ansornitinib (compound I) (25 mg/kg, p.o., twice a day, 4 weeks) can reduce fibrosis in TGFβ positive female mice[1].
Ansornitinib (compound I) (5-45 mg/kg, p.o., twice a day, 4 days) can reduce inflammatory bowel disease (IBD) in TNBS-induced IBD/acute colitis male CD-1 mice[1].
| Animal Model: | 8-10 weeks TGFβ positive female mice[1] | | Dosage: | 25 mg/kg | | Administration: | Oral administration; twice a day; 4 weeks | | Result: | Reduced lung fibrosis score, lung hydroxyproline levels and αSMA, a marker of early pulmonary fibrosis. |
| Animal Model: | TNBS-induced IBD/acute colitis male CD-1 mice[1] | | Dosage: | 5, 15, 45 mg/kg | | Administration: | Oral administration; twice a day; 4 days | | Result: | Improved colonic histology and reduced the TNBS-induced loss of cupped cells at 15 mg/kg and 45 mg/kg significantly.
Reduced the expression level of myeloperoxidase (MPO) at 5 mg/kg and 15 mg/kg significantly while there was no statistical difference at 45 mg/kg.
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| Animal Model: | Male Sprague Dawley rats[1] | | Dosage: | 30 mg/kg | | Administration: | Intravenous injection; once | | Result: | The pharmacokinetic parameters of Ansornitinib (compound I)
| Parameter | Ansornitinib (compound I) | | t1/2 | 4.1 h | | Tmax | 0.518 h | | Cmax | 7860 ng/mL | | Clearance | 173 mL/kg/min | | steady-state volume | 18.2 L/kg | | AUC0-last | 3180 ng/mL*h | | AUC0?inf_obs | 3200 ng/mL*h | |
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| [References]
[1] Shakil ASLAM, et al. Reducing fibrosis and treating related diseases, disorders, and conditions. WO2022006278 |
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