Bendamustine是一种 DNA 交联剂，能够激活 DNA 损伤反应和细胞凋亡，具有抗癌和抗代谢活性。
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Bendamustine (SDX-105 free base), a purine analogue, acts as a DNA cross-linking agent, activating DNA-damage stress response and apoptosis. It possesses potent alkylating, anticancer, and antimetabolite properties [1].
体内研究
Bendamustine (25 mg/kg, i.v.) exhibits significant inhibition of tumor cell growth, reducing it by 91%, 99%, and 95% in the DoHH-2, Granta 519, and RAMOS models, respectively. Additionally, the combination of bendamustine with rituximab enhances its antitumor effect in the DoHH-2 and RAMOS models, but not in the Granta 519 model [3].
体外研究
Bendamustine acts as a DNA cross-linking agent, inducing DNA breaks, and possesses alkylating and antimetabolite properties. It uniquely modulates apoptosis and DNA repair pathways in non-Hodgkin's lymphoma cells. At a concentration of 50 μM, bendamustine induces the expression of p21 (Cip1/Waf1) and NOXA genes, while also increasing p53 expression in SU-DHL-1 cells. Additionally, at 25 μM, bendamustine disrupts mitotic checkpoints, leading to mitotic catastrophe [1].
Bendamustine decreases the viability of multiple myeloma (MM) cell lines, including RPMI-8226 and 8226-LR5 cells, with IC25 values of 101.8 μM and 585.5 μM after 24 hours of incubation, and 51.7 μM and 374.3 μM after 48 hours of incubation, respectively. It triggers a caspase-dependent cell death pathway specific to MM cells and inhibits the spindle-assembly checkpoint [2].
Bendamustine 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK293T cells
20, 10, 5 µM
48 hours
Detect the transcriptional activation effect of VDR on the CYP24A1 promoter
J Hematol Oncol. 2017 Jun 20;10(1):127.
THP-1 cells
100 µM
2 hours
Validate the binding of Vitexin to VDR protein through CETSA and DARTS experiments
J Hematol Oncol. 2017 Jun 20;10(1):127.
T98G
5.5-65.3 μM
BDM retains its cytotoxic activity against both MGMT negative and TMZ-resistant cell lines
J Hematol Oncol. 2018 Feb 27;11(1):32.
U251MG
5.5-65.3 μM
BDM retains its cytotoxic activity against both MGMT negative and TMZ-resistant cell lines
J Hematol Oncol. 2018 Feb 27;11(1):32.
U87MG
5.5-65.3 μM
BDM retains its cytotoxic activity against both MGMT negative and TMZ-resistant cell lines
J Hematol Oncol. 2018 Feb 27;11(1):32.
KARPAS-422
200 µM
1.5 days
To evaluate the cytotoxicity of Bendamustine on DLBCL cells, results showed significant inhibition of cell viability.
J Immunother Cancer. 2024 Nov 9;12(11):e009212.
SU-DHL2
200 µM
1.5 days
To evaluate the cytotoxicity of Bendamustine on DLBCL cells, results showed significant inhibition of cell viability.
J Immunother Cancer. 2024 Nov 9;12(11):e009212.
OCI-LY1
200 µM
1.5 days
To evaluate the cytotoxicity of Bendamustine on DLBCL cells, results showed significant inhibition of cell viability.
J Immunother Cancer. 2024 Nov 9;12(11):e009212.
CLL-B cells
0.1, 30, 90 μM
48 hours
Evaluated cytotoxic effects of bendamustine combined with m15-IgG1 antibody, showing synergistic effects in both high- and low-risk CLL patients.
J Hematol Oncol. 2017 May 19;10(1):112.
Bendamustine 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SCID or SCID-bg mice
Xenograft models of non-Hodgkin’s lymphoma
Intravenous injection
25 mg/kg
Single dose
To evaluate the efficacy of Bendamustine alone or in combination with rituximab in non-Hodgkin’s lymphoma models. Results showed that Bendamustine exhibited significant activity in all tested tumor models, with enhanced effects when combined with rituximab.
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