DB2313

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DB2313 是一种有效的转录因子 PU.1 抑制剂，IC50=14 nM。 DB2313 破坏 PU.1 与靶基因启动子的相互作用。 DB2313 诱导急性髓系白血病 (AML) 细胞凋亡，并具有抗癌作用

DB2313 is a potent transcription factor PU.1 inhibitor, IC50=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(In Vitro):DB2313 decreases PU.1 occupancy on E2f1, Junb, and Csf1r promoters in AML cells. 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. (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.

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.In AML cells, DB2313 decreases PU.1 occupancy on E2f1, Junb, and Csf1r promoters.

DB2313 (17 mg/kg; i.p.; three times per week; for 3 weeks) treatment decreases leukemia progression and results in increased survival in mice. Animal Model:NSG mice bearing sublethally irradiated (2.0 Gy) and injection with PU.1 URE–/– AML cells Dosage:17 mg/kg Administration:Intraperitoneal injection; three times per week; for 3 weeks Result:Decreased tumor burden and resulted in increased survival.

Carboximidamide

Apoptosis

Apoptosis

5-HT2C|5-HT2A|5-HT2B

——

——

2170606-74-1

708.83

C42H41FN8O2

>98% (HPLC)

In Vitro:?DMSO : 3.7 mg/mL (5.22 mM)

——

——

(-20℃)

With Ice Pack

≥ 2 years