SG-55
SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP+), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC).
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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。
- 分子式: C19H17N3O2
- 分子量:319.36
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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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AKR1C3 5 nM (IC50) |
AKR1C3 10 nM (IC50) |
SG-55 (0.5-100 μM; 72 h) does not inhibits the cell growth of AKR1C3-overexpressing PC-9/OR cell line (PC-9 EGFR 19Del/T790M/C797S cells)[1].
SG-55 (72 h) at 10 μM, 20 μM and 50 μM decreased the IC50 of Osimertinib (100-500 nM) in PC-9/OR cells from 2.59 μM to 1.30 μM, 0.43 μM and 0.23 μM, respectively, corresponding to resistance-reversal factors of 2, 6 and 11-fold[1].
SG-55 (10 μM) cooperates with Osimertinib to suppress clonogenicity (14 days), curtail migration (24 h), and amplify cycle arrest (24 h) and apoptosis (72 h), thereby conferring significant sensitization in PC-9/OR cells[1].
SG-55 (10 μM; 72 h)-mediated AKR1C3 inhibition elevates the NADPH/NADP+ ratio, disrupts the GSH cycle, breaks redox balance, and amplifies oxidative damage, thereby overcoming EGFR mutation-driven Osimertinib resistance in PC-9/OR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AKR1C3-overexpressing PC-9/OR cell lines
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Concentration:10 μM plus Osimertinib (100 nM)
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Incubation Time:72 h
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Result:AKR1C3 Inhibition enhanced Osimertinib-induced apoptosis.
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Cell Line:AKR1C3-overexpressing PC-9/OR cell lines
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Concentration:10 μM plus Osimertinib (100 nM)
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Incubation Time:24 h
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Result:Osimertinib alone imposed a G0/G1 arrest, whereas the addition of the compound shifted the cycle distribution to G2/M accumulation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c nude mice (6 weeks old) were inoculated subcutaneously in the right flank with 3 × 107 PC-9/OR cells (100 μL) to establish xenografts[1].
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Dosage:10 mg/kg plus Osimertinib (5 mg/kg p.o.)
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Administration:p.o.; every 1 days; for 21 days
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Result:The tumor-growth inhibition (TGI) values of 15.6%.
When used in combination with osimertinib, the TGI was 93.1%.
No significant body-weight loss was observe.
化学情報
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分子量 319.36
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分子式 C19H17N3O2
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SMILES
N#CC1=CC2=C(C=C1)CN(C(C3=CC(C(C4CC4)=O)=CN3)=O)CC2
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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)
SG-55 関連分類
HY-181542 関連分類
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