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The effect of Gö6976 on chronic myeloid leukemia in vitro and in vivo.

Abstract：

:Objectives: Chronic myeloid leukemia (CML) is a malignant tumor of the blood system. Gö6976, as a type of indolocarbazole and shows strong antitumor effects, but there have been no reports on the effect of Gö6976 on CML. The objectives of this research were: (1) to explore the impact of Gö6976 on CML in vitro and in vivo; and (2) to explore the drug toxicity of Gö6976 to normal cells and animals.Methods:K562 cells and CML mice were used to explore the effect of Gö6976 on CML. Peripheral blood mononuclear cells (PBMCs), CD34+ cells, and healthy mice were used to explore the drug toxicity of Gö6976.Results: Cell experiments showed that Gö6976 could inhibit the proliferation of K562 cells and enhance the inhibitory effects of imatinib at 5 μM and 10 μM, but it had little effect on CD34+ cells or PBMCs at concentrations less than 5 μM. Animal experiments showed that 2.5 mg/kg Gö6976 could effectively inhibit the development of CML in mice, and it had almost no effects on healthy mice at 2.5 mg/kg and 10 mg/kg.Discussion: Because of the direct inhibitory effect of Gö6976 on CML and its pharmacological enhancement effect on imatinib, it is foreseeable that Gö6976 could become a new type of anti-CML medicine. And the further research is needed.Conclusion: Our findings verified that Gö6976 could effectively inhibit CML in vitro and in vivo, and it is almost nontoxic to hematopoietic cells, immune cells, and healthy mice.

journal_name

Hematology

journal_title

Hematology (Amsterdam, Netherlands)

authors

Cao ZR,Chen XP,Feng M,Hou YL,Li Y,Hu XL,Huang ZL,Hu J

doi

10.1080/16078454.2021.1945235

keywords:

["310.4710","320.2430","Gö6976","K562","chronic myeloid leukemia","toxicity"]

subject

Has Abstract

pub_date

2021-12-01 00:00:00

pages

543-551

issue

1

eissn

1024-5332

issn

1607-8454

journal_volume

26

pub_type

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