OICR19451
OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC50 values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer.
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- CAS No.: 2803349-61-1
- Formule: C26H31ClF2N8O2S
- Masse moléculaire:593.09
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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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Activité biologique
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NUAK1 12 nM (IC50) |
NUAK2 10 nM (IC50) |
MARK2 101 nM (IC50) |
MARK3 124 nM (IC50) |
OICR19451 modulates Hippo pathway activity in MDA-MB-231 cells, increasing YAP phosphorylation (EC50 = 125 nM), driving cytoplasmic YAP/TAZ localization (EC50 = 144 nM), and inhibiting cell growth (EC50 = 202 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID-gamma (NSG) (female, 10 weeks old)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Inhibited tumor growth relative to controls.
Prolonged survival relative to controls.
Reduced metastasis to peritoneal space (mesentery) and liver relative to controls.
Decreased YAP/TAZ protein levels in tumors (60 mg/kg group).
Induced widespread tumor necrosis and collagenous tumor encapsulation.
Caused acceptable, reversible body weight loss with no gross behavioral or CNS-related side effects.
Chemical Information
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CAS No. 2803349-61-1
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Masse moléculaire 593.09
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Formule C26H31ClF2N8O2S
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SMILES
CN1CCN(CC1)C2CCN(CC2)C3=CC(OC(F)F)=C(C=C3)NC4=NC=C(C(NC5=C(SC=C5)C(N)=O)=N4)Cl
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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)
OICR19451 Related Classifications
HY-182743 Related Classifications
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