Axl-IN-17
Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy.
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- CAS. Nr.: 3048409-80-6
- Formel: C32H27F2N7O
- Molecular Weight:563.60
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
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Axl |
Axl 3.23 nM (IC50) |
Mer |
Tyro3 |
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Cell Line
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Type | Value | Description | References |
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| MKN-45 | IC50 |
>100 nM
Compound: 13c
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Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
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[PMID: 38128234] |
Axl-IN-17 inhibits cancer-related kinases TYRO3, MER, MET, RON at 1 μM[1].
Axl-IN-17 exhibits antiproliferative activities in BaF3/TEL-AXL cell, with IC50 value <1 nM[1].
Axl-IN-17 (1 nM, 2 h) inhibits phosphorylation of AXL and its downstream signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BaF3/TEL-AXL
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Concentration:1 nM
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Incubation Time:72 h
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Result:Inhibited proliferation activity in BaF3/TEL-AXL cells.
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Cell Line:BaF3/TEL-AXL
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Concentration:1 nM
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Incubation Time:2 h
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Result:Inhibited phosphorylation of AXL and its downstream signaling
Axl-IN-17 (p.o.,25, 50 or 100 mg/kg, once daily for 7 days) exhibits antitumor efficacy in AXL-driven tumor xenograft mice[1].
Pharmacokinetic Analysis of AXL-IN-17 in Male Sprague-Dawley rats[1]
| Route | Dose (mg/kg) | AUC0→∞ (ng·h/mL) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | MRT0→∞(h) |
| p.o. | 3 mg/kg | 59815 | 10.09 | 2 | 2906 | 16.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats /pharmacokinetic[1]
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Dosage:3 mg/kg (p.o.), once daily
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Administration:Oral gavage
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Result:Revealed a T1/2 value of 10.09 h and an AUC value of 59815 ng•h/mL.
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Animal Model:BaF3/TEL-AXL xenograft mice[1]
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Dosage:25, 50 or 100 mg/kg, once daily for 7 days
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Administration:Oral gavage
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Result:Induced tumor regression.
Chemical Information
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CAS. Nr. 3048409-80-6
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Molecular Weight 563.60
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Formel C32H27F2N7O
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SMILES
CC(C)N1C=C(C2=CC=C(F)C=C2)C(C3=C(NC4=CC(F)=C(C5=C(N)N=CC(C6=CN(C)N=C6)=C5)C=C4)N=CC=C31)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Axl-IN-17 Related Classifications
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