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  2. Membrane Transporter/Ion Channel
  3. GLUT
  4. DRB18

DRB18 是一種有效的葡萄糖轉運蛋白 (GLUT) 泛抑制劑。DRB18 通過改變葡萄糖相關途徑中代謝產物的豐度來改變 A549 細胞中的能量相關代謝。DRB18 最終可導致細胞阻滯在 G1/S 期，增加氧化應激和壞死細胞死亡。DRB18 具有抗腫瘤活性。

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DRB18 Chemical Structure

DRB18 Chemical Structure

CAS No. : 2863686-81-9

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2198
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1 mg ￥1180
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5 mg ￥2610
In-stock
10 mg ￥4140
In-stock
25 mg 現(xiàn)貨 詢價
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Customer Review

查看 GLUT 亞型特異性產品:

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

生物活性

DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity[1].

IC50 & Target

GLUT[1]
細胞效力
(Cellular Effect)
Cell Line Type Value Description References
NCI-H1299 IC50
1.9 μM
Compound: 4v
Inhibition of glucose uptake in human NCI-H1299 cells incubated for 10 mins followed by L-[3H]2-deoxyglucose and glucose addition and measured after 30 mins by scintillation counting method
Inhibition of glucose uptake in human NCI-H1299 cells incubated for 10 mins followed by L-[3H]2-deoxyglucose and glucose addition and measured after 30 mins by scintillation counting method
[PMID: 32736210]
NCI-H1299 IC50
7 μM
Compound: 4v
Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 32736210]
體外研究
(In Vitro)

DRB18 (0-10 μM；30 分鐘) 以劑量依賴性方式降低表達 GLUT1-4 的 HEK293 細胞系中的葡萄糖攝取，IC50 范圍從 ~ 900 nM 到 ~ 9 μM[1]。
DRB18 (5 和 10 μM；72 小時) 導致 G1/S 期轉變中的細胞周期停滯[1]。
DRB18 (5 和 10 μM；72 小時) 增加 A549 細胞中的 ROS 水平[1]。
DRB18 (5 和 10 μM；72 小時) 降低糖基化 GLUT1 和 GLUT2-4 的表達A549細胞呈劑量依賴性[1]。

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

Cell Proliferation Assay

Cell Line: GLUT1-4-expressed HEK293 cell lines[1]
Concentration: 0-10 μM
Incubation Time: 30 min
Result: Reduced glucose uptake in these cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM.

Cell Cycle Analysis

Cell Line: A549[1]
Concentration: 5 and 10 μM
Incubation Time: 72 hours
Result: Caused cell cycle arrest in the G1/S phase transition.

Western Blot Analysis

Cell Line: A549[1]
Concentration: 5 and 10 μM
Incubation Time: 72 hours
Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.

Western Blot Analysis

Cell Line: A549[1]
Concentration: 5 and 10 μM
Incubation Time: 72 hours
Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.
體內研究
(In Vivo)

DRB18 (10 mg/kg；腹腔注射；每周三次，持續(xù) 5 周) 可抑制 44% 的腫瘤體積和 43% 的腫瘤重量[1]。

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

Animal Model: Male NU/J nude mice (3-4 weeks; tumor cell-injected)[1]
Dosage: 10 mg/kg
Administration: IP; thrice a week for 5 weeks
Result: The tumors were 44% smaller by volume and 43% smaller by weight, also showed DRB18 decreased expression of GLUT1-4 (Fig. 5f) and reduced proliferative capacity within the xenografted tumor.
分子量

382.88

Formula

C22H23ClN2O2
CAS 號
性狀

固體

顏色

White to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 50 mg/mL (130.59 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 2.6118 mL 13.0589 mL 26.1178 mL
5 mM 0.5224 mL 2.6118 mL 5.2236 mL
查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料

純度: 99.58%

參考文獻

完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6118 mL 13.0589 mL 26.1178 mL 65.2946 mL
5 mM 0.5224 mL 2.6118 mL 5.2236 mL 13.0589 mL
10 mM 0.2612 mL 1.3059 mL 2.6118 mL 6.5295 mL
15 mM 0.1741 mL 0.8706 mL 1.7412 mL 4.3530 mL
20 mM 0.1306 mL 0.6529 mL 1.3059 mL 3.2647 mL
25 mM 0.1045 mL 0.5224 mL 1.0447 mL 2.6118 mL
30 mM 0.0871 mL 0.4353 mL 0.8706 mL 2.1765 mL
40 mM 0.0653 mL 0.3265 mL 0.6529 mL 1.6324 mL
50 mM 0.0522 mL 0.2612 mL 0.5224 mL 1.3059 mL
60 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0882 mL
80 mM 0.0326 mL 0.1632 mL 0.3265 mL 0.8162 mL
100 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6529 mL
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.

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產品名稱：
DRB18
目錄號：
HY-145963
需求量：