Belapectin

Names

[ CAS No. ]:
1980787-47-0

[ Name ]:
Belapectin

Biological Activity

[Description]:

Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer

[Target]

Ki: 2.8 μM (Galectin-3)[2]


[In Vitro]

Belapectin (0.2 mg/mL, 2 mg/mL; 48 h) 抑制 4T1 和 MCA-205 细胞的增殖，诱导凋亡[1]。 Apoptosis Analysis[1] Cell Line: TRAMP-C1, 4T1 and MCA-205 cells Concentration: 0.2 mg/mL, 2 mg/mL Incubation Time: 48 h Result: Decreased the proliferation and resulted a minimal increase in apoptosis of 4T1 and MCA-205 cells. But showed no impact on TRAMP-C1 cell.

[In Vivo]

Belapectin (2.4 mg/mouse; 腹腔注射; 每周 3 次, 共 3 周) 仅与 anti-OX40 mAb 联合处理后，才导致肿瘤生长显著减少、存活率相应增加。联合处理还产生了持久的长期记忆，100% 无瘤小鼠被保护免于随后的肿瘤再攻击[1]。 Animal Model: Wild-type C57BL/6 and BALB/c mice[1] Dosage: 2.4 mg/mouse, accompanied with anti-OX40 mAb (250 µg) Administration: Intraperitoneal injection; 3 times per week for 3 weeks Result: Inhibited tumor growth. Enhanced the efficacy of checkpoint blockade (aPD-L1) immunotherapy.

[References]

[1]. Sturgill ER, et al. Galectin-3 inhibition with belapectin combined with anti-OX40 therapy reprograms the tumor microenvironment to favor anti-tumor immunity. Oncoimmunology. 2021 Mar 1;10(1):1892265.  

[2]. Capasso D, et al. Galectins detection for the diagnosis of chronic diseases: An emerging biosensor approach[J]. TrAC Trends in Analytical Chemistry, 2023: 116952.

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds

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