DB2313

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

DB2313  纯度: 98.13%

DB2313 是一种有效的转录因子 PU.1 抑制剂,apoptosis 为 14 nM。DB2313 破坏了 PU.1 与靶基因启动子的相互作用。DB2313 可诱导急性髓细胞性白血病 (AML) 细胞凋亡 (apoptosis),并具有抗癌作用。

DB2313

DB2313 Chemical Structure

CAS No. : 2170606-74-1

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DB2313 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

DB2313 is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects[1].

IC50 & Target

IC50: 14 nM (PU.1)[1]

体外研究
(In Vitro)

DB2313 treatment leads to a profound decrease in the growth of PU.1 URE–/– acute myeloid leukemia (AML) cells (IC50 of 7.1 μM), while showing little effect on normal hematopoietic cells at similar concentrations. DB2313 treatment leads to a 3.5-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells. DB2313 also leads to a significant decrease in clonogenicity in the second and third rounds of plating and a complete disruption of clonogenic capacity in the fourth and higher rounds of plating[1].
In AML cells, DB2313 decreases PU.1 occupancy on E2f1, Junb, and Csf1r promoters[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

DB2313 (17 mg/kg; i.p.; three times per week; for 3 weeks) treatment decreases leukemia progression and results in increased survival in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NSG mice bearing sublethally irradiated (2.0 Gy) and injection with PU.1 URE–/– AML cells[1]
Dosage: 17 mg/kg
Administration: Intraperitoneal injection; three times per week; for 3 weeks
Result: Decreased tumor burden and resulted in increased survival.

分子量

708.83

Formula

C42H41FN8O2

CAS 号

2170606-74-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 3.7 mg/mL (5.22 mM; ultrasonic and warming and heat to 70°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4108 mL 7.0539 mL 14.1078 mL
5 mM 0.2822 mL 1.4108 mL 2.8216 mL
10 mM

*

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。

参考文献
  • [1]. Iléana Antony-Debré, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017 Dec 1;127(12):4297-4313.

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