pelcitoclax

small molecule inhibitor of BCL-2/BCL-XL

Also Known As:

3-(1-((3R)-3-(4-((4-(4-(3-(2-(4-chlorophenyl)-5-methyl-4-methylsulfonyl-1-propan-2-ylpyrrol-3-yl)-5-fluorophenyl)piperazin-1-yl)phenyl)sulfamoyl)-2-(trifluoromethylsulfonyl)anilino)-4-phenylsulfanylbutyl)piperidine-4-carbonyl)oxypropylphosphonic acid; APG 1252; APG-1252; APG1252

Networked: 3 relevant articles (1 outcomes, 2 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Cao, Jia-Xin: 1 article (01/2021)
2.	Lu, Fei-Teng: 1 article (01/2021)
3.	Luo, Fan: 1 article (01/2021)
4.	Luo, Min: 1 article (01/2021)
5.	Luo, Qiu-Yun: 1 article (01/2021)
6.	Ma, Wen-Juan: 1 article (01/2021)
7.	Pan, Wen-Tao: 1 article (01/2021)
8.	Qiu, Miao-Zhen: 1 article (01/2021)
9.	Xia, Zeng-Fei: 1 article (01/2021)
10.	Yang, Da-Jun: 1 article (01/2021)

Related Diseases

1.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 11/01/2022 - "Therapeutic potential of the novel Bcl-2/Bcl-XL dual inhibitor, APG1252, alone or in combination against non-small cell lung cancer." 11/01/2022 - "This study focused on evaluating the therapeutic efficacy of the novel Bcl-2/Bcl-XL dual inhibitor, APG1252-M1 (also named APG-1244; an in vivo active metabolite of APG1252 or pelcitoclax), as a single agent or in combination, against non-small cell lung cancer (NSCLC) cells. "
2.	Neoplasms (Cancer) 11/16/2023 - "First-in-Human Study with preclinical data of BCL-2/BCL-xL Inhibitor Pelcitoclax in Locally Advanced or Metastatic Solid Tumors." 11/16/2023 - "Our data demonstrate that pelcitoclax has antitumor activity and is well tolerated, supporting its further clinical development for human solid tumors, particularly combined with agents that downregulate MCL-1." 11/16/2023 - "Levels of BCL-xL complexes correlated with tumor growth inhibition by pelcitoclax. " 11/16/2023 - "Subjects (N = 50) with metastatic small cell lung cancer and other solid tumors received intravenous pelcitoclax once or twice weekly. " 11/16/2023 - "Pelcitoclax exhibited strong BAX/BAK‒dependent and caspase-mediated antiproliferative and apoptogenic activity in various cancer cell lines. "
3.	Small Cell Lung Carcinoma (Small Cell Lung Cancer) 11/16/2023 - "Subjects (N = 50) with metastatic small cell lung cancer and other solid tumors received intravenous pelcitoclax once or twice weekly. "
4.	Stomach Neoplasms (Stomach Cancer) 11/16/2023 - "Consistent with cell- based apoptogenic activity, pelcitoclax disrupted BCL-xL:BIM and BCL-xL:PUMA complexes in lung and gastric cancer PDX models. "
5.	Nasopharyngeal Carcinoma 01/01/2021 - "Gemcitabine and APG-1252, a novel small molecule inhibitor of BCL-2/BCL-XL, display a synergistic antitumor effect in nasopharyngeal carcinoma through the JAK-2/STAT3/MCL-1 signaling pathway."

Related Drugs and Biologics

1.	pelcitoclax
2.	Caspases
3.	Gemcitabine