Busulfan

CAS No. : 55-98-1

MCE 国际站：Busulfan

产品活性：Busulfan 是一种有效的烷化抗肿瘤剂，通过交联 DNA 以及 DNA 和蛋白质造成 DNA 损伤。Busulfan 抑制硫氧还蛋白还原酶，也可以诱导细胞凋亡。Busulfan 是一种免疫抑制和清髓性化疗活性分子。

研究领域：Cell Cycle/DNA Damage | Apoptosis

作用靶点：DNA Alkylator/Crosslinker | Apoptosis

In Vitro: Busulfan (120 μM; 24 h) incited a moderate p53 activation, but strong Erk, p38, and JNK phosphorylation, in a time-dependent manner.
Busulfan (120 μM; 24 h) results in premature senescence in WI38 cells via the Erk and p38 MAPK pathway, reduces GSH and increases ROS production, but the production can be suppressed by NADPH oxidase.

In Vivo: Busulfan can be used in animal modeling to establish models of acute aplastic anemia. Busulfan (40 mg/kg; i.p; single dose) increases apoptosis and decreases the testis weight in mice.
Busulfan (2.5, 5.0 mg/kg, i.p.) causes earlier occurrence of persistent esturs in a dose dependent manner in rats. Busulfan (5.0 mg/kg) also increases the incidence of uterine adenocarcinomas and multiplicity of uterine neoplastic lesions.
AUC is 220 ± 34 h·nmol·mL^-1 after 16.5 mg/kg and 604 ± 87 h·nmol·mL^-1 after 33 mg/kg at the first injection in mice.

Induction of aplastic anemia model

Background

Busulfan causes DNA damage by cross-linking DNA as well as DNA and proteins.

Specific Mmodeling Methods

ICR mice : male • 18-22 g, 6-8 weeks
Administration: 20 mg/kg busulfan+40 mg/kg cyclophosphamide• i.p. • one time per day for 12 days.

Note

(1) Twenty-four hours after the last intraperitoneal injection, tail vein blood was collected from eight mice randomly selected from each group for blood test.
(2) the mice are sacrificed by cervical dislocation and one femur was surgically dissected. After removing epiphysis from the femur, bone marrow cells are washed off using 1 ml PBS to prepare bone marrow cell suspension.

Modeling Record

The peripheral blood cells, hemoglobin, and bone marrow nucleated cells decreased significantly.
Histopathological: the proliferation of bone marrow hematopoietic tissues and cells was inhibited, and non-hematopoietic cells (fat cells) were significantly increased.

Correlated Product(s): Cyclophosphamide (HY-17420)

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