UNC3133
UNC3133 is an orally active, limitedly selective MerTK inhibitor with an IC50 of 3.0 nM. UNC3133 inhibits Axl, Tyro3 and Flt3 kinases, with IC50 values of 17 nM, 31 nM and 6.8 nM, respectively. UNC3133 is applicable to the research of inflammatory diseases and cancers.
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- CAS No.: 2011034-35-6
- Formule: C30H44N6O
- Masse moléculaire:504.71
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Axl 17 nM (IC50) |
MERTK 3.0 nM (IC50) |
Tyro3 31 nM (IC50) |
FLT3 6.8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
110 nM
Compound: 16
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Inhibition of human MerTK kinase domain (1585 to 3000 residues) expressed in HEK293 cells co-expressing rat EGFR LBD assessed as inhibition of EGF-stimulated MerTK phosphorylation preincubated for 30 mins followed by EGF stimulation for 15 mins by ELISA
Inhibition of human MerTK kinase domain (1585 to 3000 residues) expressed in HEK293 cells co-expressing rat EGFR LBD assessed as inhibition of EGF-stimulated MerTK phosphorylation preincubated for 30 mins followed by EGF stimulation for 15 mins by ELISA
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[PMID: 27994735] |
UNC3133 potently inhibits purified MerTK kinase activity with an IC50 of 3.0 nM, while also inhibiting Axl, Tyro3, and Flt3 kinases with IC50 values of 17 nM, 31 nM, and 6.8 nM, respectively[1].
UNC3133 inhibits EGF-stimulated MerTK phosphorylation in HEK293 cells expressing an EGFR-MerTK chimeric protein with an EC50 of 110 nM[1].
UNC3133 (300 nM) demonstrates limited kinome selectivity, with greater than 50% inhibition of 12 kinases when tested at 300 nM, including eight tyrosine kinases and four serine/threonine kinases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2011034-35-6
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Masse moléculaire 504.71
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Formule C30H44N6O
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SMILES
OC(CCCCCCCN1)CCCCN2C3=NC1=NC=C3C(C4=CC=C(C=C4)CN5CCN(CC5)C)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UNC3133 Related Classifications
HY-115778 Related Classifications
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