PBD-2131 causes apoptosis in cancer cells

Key technology

Our proprietary compounds have shown strong anti-cancer effects against various types of cancers with minimal toxicity in both in vitro and in vivo models. They induce apoptosis in cancer cells, especially in MDR cancers.  They also arrest cell proliferation and induced cell differentiation at lower doses.


 

Lower dose PBD-2131 induced cancer cells differentiation
Lower dose PBD-2131 causes G1 arrest

Caspase pathway in cancer cells is activated and the permeability of mitochondria membrane is changed, causing cytochrome C release. The figure1 below shows cancer cells treated with PBD-2131 and stained for a mitochondrial membrane permeability indicator. The green cells are those with “leaking” mitochondria. The figure2 below shows the amount of activated caspase is induced with increasing doses. A, B, C, and D represent the samples collected from the cells treated with PBD-2131 at concentration of 50,20,10 and 0 µg/ml, respectively. 

 
Figure1
Figure2

The Intracranial Glioma Anima Model illustrates cancer inhibitory effect of PBD-2131 in vivo.

Intracranial Glioma Animal Model:
Survival Curve
Intracranial Glioma Animal Model:
Tumor Response

The cancer cells tested are listed below, in all of which PBD-2131 and its active ingredients have shown anti-cancer efficacy.

Pancreatic cancer:   BXPC-3, Capan-1, MIAPaCa
Breast cancer: MCF7, MCF7adr, MDA435LCC6M, MDA435LCC6W
Brain cancer: U87, U87delta, 9L, SF188, SF120, SF210, U126, U373
Prostate cancer: LNCaP, PC3
Intestinal cancer: HCT15
Gastric cancer: Keto
Melanoma: B16, MMRU, SK-mel-110
Lung cancer: H460, MS-1, H838
Liver cancer: H22
Sarcoma: S180
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