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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2803349-61-1
- 分子式: C26H31ClF2N8O2S
- 分子量:593.09
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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.
化学情報
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CAS 番号 2803349-61-1
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分子量 593.09
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
OICR19451 関連分類
HY-182743 関連分類
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