Aurora B/RET-IN-1
Aurora B/RET-IN-1 is a dual RET and Aurora B inhibitor with human IC50 values of 78 nM and 24 nM, respectively. Aurora B/RET-IN-1 binds the DFG-out conformation of RET as a type II inhibitor and extends into the allosteric pocket. Aurora B/RET-IN-1 inhibits Aurora B kinase activity. Aurora B/RET-IN-1 inhibits RET and Aurora B signaling pathways. Aurora B/RET-IN-1 can be used for research on non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C32H36F3N9O
- Molecular Weight:619.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Aurora Kinase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Ret 78 nM (IC50) |
Aurora B 24 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LC-2-ad | IC50 |
0.14 μM
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Cytotoxicity against human LC-2/ad NSCLC cells assessed as reduction in cell viability by MTT assay.
Cytotoxicity against human LC-2/ad NSCLC cells assessed as reduction in cell viability by MTT assay.
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42648234 |
In Vitro
Aurora B/RET-IN-1 is a type II RET inhibitor that binds to the DFG-out conformation of RET[1].
Aurora B/RET-IN-1 is a potent dual inhibitor of RET and Aurora B kinases with IC50 values of 0.078 μM and 0.024 μM, respectively[1].
Aurora B/RET-IN-1 (10-80 min) acts as a type II RET inhibitor, with its potency increasing over time[1].
Aurora B/RET-IN-1 (0.1-5 μM; 2 h) inhibits the phosphorylation of both RET and Histone H3 in LC-2/ad cells, supporting its dual-target mechanism[1].
Aurora B/RET-IN-1 (Compound 47) exhibits potent cytotoxicity against the RET-driven LC-2/ad NSCLC cell line with an IC50 of 0.14 μM[1].
Aurora B/RET-IN-1 (0.004-1 μM; 15 days) inhibits colony formation in LC-2/ad cells[1].
Aurora B/RET-IN-1 displays greater than 30-fold selectivity for the RET-driven LC-2/ad cell line over RET-independent A549 and H1975 cells[1].
Aurora B/RET-IN-1 exhibits greater than 20-fold selectivity for LC-2/ad cells over normal fibroblasts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LC-2/ad
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Concentration:0.004 μM; 0.012 μM; 0.037 μM; 0.11 μM; 0.33 μM; 1 μM
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Incubation Time:15 days
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Result:Inhibited colony formation of LC-2/ad cells.
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Cell Line:LC-2/ad
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Concentration:0.1 μM, 0.5 μM, 1 μM, and 5 μM
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Incubation Time:2 h
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Result:Resulted in a dose-dependent reduction in phospho-Histone H3 levels.
Reduced the phosphorylation of both RET and Histone H3 at tested concentrations up to 5 μM.
Chemical Information
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Molecular Weight 619.68
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Formula C32H36F3N9O
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SMILES
CC(C)N(C(C)C)CCN1N=CC(C(C=C2)=CC3=C2C(NC4=CC=C(CC(NC5=CC(C(F)(F)F)=NN5C)=O)C=C4)=NC=N3)=C1
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Aurora B/RET-IN-1 Related Classifications
HY-189295 Related Classifications
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