GZD-257
GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM).
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- 分子式: C26H29ClN6O4
- 分子量:525.00
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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
GZD-257 (Compound 7) shows potent activity against glioma cell lines U118-MG (IC50 = 1.64 μM) and U87-MG (IC50 = 1.40 μM), and lower potency against LO2 cells (IC50 = 9.35 μM)[1].
GZD-257 (10 μM, 16 h) shows a permeability coefficient (Pe) of 43.85× 10-6 cm/s, demonstrating excellent blood-brain barrier penetration ability[1].
GZD-257 (1-20 μM, 24 h) induces late apoptosis in a concentration-dependent manner in U118-MG cells[1].
GZD-257 (1-20 μM) causes G2/M phase arrest, with the proportion increasing from 10.38 % to 67.19 % in U118-MG cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U118-MG cells
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Concentration:1 μM, 5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Induces late apoptosis in a concentration-dependent manner: 8.42 % at 1 μM, 9.65 % at 5 μM, 11.6 % at 10 μM, and 36.8 % at 20 μM.
化学情報
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分子量 525.00
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分子式 C26H29ClN6O4
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SMILES
ClC(C=N1)=C(NC2=CC3=CC=C2C(NC)=O)N=C1NC(C=C4)=CC(OCCCCO3)=C4N5CCOCC5
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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)
GZD-257 関連分類
HY-178969 関連分類
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