DRB18|西域试剂

DRB18,98.81%

产品编号：Bellancom-145963| 分子式：C₂₂H₂₃ClN₂O₂| 分子量：382.88

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货号	价格	库存与货期
Bellancom-145963	￥2900.00	杭州北京（现货）
Bellancom-145963	￥4600.00	杭州北京（现货）
Bellancom-145963	￥9200.00	杭州北京（现货）
Bellancom-145963	￥14800.00	杭州北京（现货）

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DRB18

产品介绍

DRB18 是一种有效的葡萄糖转运蛋白 (GLUT) 泛抑制剂。DRB18 通过改变葡萄糖相关途径中代谢产物的丰度来改变 A549 细胞中的能量相关代谢。DRB18 最终可导致细胞阻滞在 G1/S 期，增加氧化应激和坏死细胞死亡。DRB18 具有抗肿瘤活性。

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.

体外研究

DRB18 (0-10 μM; 30 min) reduces glucose uptake in GLUT1-4-expressed HEK293 cell lines in a dose-dependent manner with IC₅₀s varying from ~ 900 nM to ~ 9 μM.
DRB18 (5 and 10 μM; 72 hours) causes cell cycle arrest in the G1/S phase transition.
DRB18 (5 and 10 μM; 72 hours) increases ROS levels in A549 cells.
DRB18 (5 and 10 μM; 72 hours) reduces expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.

西域 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
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
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
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
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.

体内研究
(In Vivo)

DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43%.

西域 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)
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.

体内研究

DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43%.

西域 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)
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.

体内研究

DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43%.

西域 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)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (130.59 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	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
10 mM	0.2612 mL	1.3059 mL	2.6118 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式