2. Metabolic Enzyme/Protease
  3. Aldose Reductase
  4. SG-55

SG-55 是一种选择性非竞争性且具有口服活性的 AKR1C3 抑制剂，IC50 为 5 nM，Ki 为 10 nM。SG-55 对 AKR1C3 的选择性比对 AKR1C1、AKR1C2 和 AKR1C4 的选择性高 2000 倍以上 (> 10 μM)。 SG-55 可提高还原型/氧化型烟酰胺腺嘌呤二核苷酸磷酸 (NADPH/NADP+) 的比值，降低还原型/氧化型谷胱甘肽 (GSH/GSSG) 的比值，并诱导 DNA 双链断裂。SG-55 可克服非小细胞肺癌 (NSCLC) 中由 EGFR C797S 三重突变介导的 Osimertinib (HY-15772) 耐药性。

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SG-55

SG-55 Chemical Structure

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Customer Review

SG-55 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)[1].

IC50 & Target[1]

AKR1C3

5 nM (IC50)

AKR1C3

10 nM (Ki)

体外研究
(In Vitro)

SG-55 (0.5-100 μM; 72 h) 不抑制 AKR1C3 过表达的 PC-9/OR 细胞系 (PC-9 EGFR 19Del/T790M/C797S 细胞) 的细胞生长[1]。
SG-55 (72 小时) 在 10 μM、20 μM 和 50 μM 浓度下，可分别将 PC-9/OR 细胞中 Osimertinib (100-500 nM) 的 IC50 值从 2.59 μM 降低至 1.30 μM、0.43 μM 和 0.23 μM，对应的耐药性逆转倍数分别为 2 倍、6 倍和 11 倍[1]。
SG-55 (10 μM) 与 Osimertinib 协同作用，可抑制克隆形成 (14 天)、减缓细胞迁移 (24 小时)，并增强细胞周期阻滞 (24 小时) 和凋亡 (72 小时)，从而显著提高 PC-9/OR 细胞的药物敏感性[1]。
SG-55 (10 μM; 72 h) 介导的 AKR1C3 抑制可提高 NADPH/NADP+ 比值，破坏 GSH 循环，打破氧化还原平衡，并加剧氧化损伤，从而克服 PC-9/OR 细胞中由 EGFR 突变驱动的 Osimertinib 耐药性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SG-55 相关抗体:

Apoptosis Analysis[1]

Cell Line: AKR1C3-overexpressing PC-9/OR cell lines
Concentration: 10 μM plus Osimertinib (100 nM)
Incubation Time: 72 h
Result: AKR1C3 Inhibition enhanced Osimertinib-induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: AKR1C3-overexpressing PC-9/OR cell lines
Concentration: 10 μM plus Osimertinib (100 nM)
Incubation Time: 24 h
Result: Osimertinib alone imposed a G0/G1 arrest, whereas the addition of the compound shifted the cycle distribution to G2/M accumulation.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax
Rat[1] 10 mg/kg p.o. 280011.39 μg/L
Rat[1] 2 mg/kg i.v. 22371.51 μg/L
体内研究
(In Vivo)

SG-55 (10 mg/kg；口服；每日一次；持续 21 天) 可显著降低小鼠体内 Osimertinib 耐药的 EGFR C797S 肿瘤的密度[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 10 mg/kg plus Osimertinib (5 mg/kg p.o.)
Administration: p.o.; every 1 days; for 21 days
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.
分子量

319.36

Formula

C19H17N3O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SG-55 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SG-55SG55SG 55Aldose ReductaseAKR1C3 inhibitornoncompetitiveNADPH/NADP+GSH/GSSGOsimertinib resistancenon-small cell lung cancer (NSCLC)EGFR 19Del/T790M/C797SInhibitorinhibitorinhibit

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目录号：
HY-181542
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