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.
For research use only. We do not sell to patients.
- CAS No.: 3048409-80-6
- Formula: C32H27F2N7O
- Molecular Weight:563.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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Axl |
Axl 3.23 nM (IC50) |
Mer |
Tyro3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
In Vitro
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. Further protocols information, click here.
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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
In Vivo
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 No. 3048409-80-6
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Molecular Weight 563.60
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Axl-IN-17 Related Classifications
HY-162085 Related Classifications
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