MCE products for research use only. We do not sell to patients.

Dasminapant

MCE China：Dasminapant

Brand：MedChemExpress (MCE)

Cat. No.HY-125593

CAS：1570231-89-8

Synonyms：APG-1387

Purity：99.36%

Storage：-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.

In Vitro：Dasminapant (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells[1]. Dasminapant (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. Dasminapant sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro[1].

In Vivo：Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice[1]. Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) monotherapy exhibits some degree of anti-tumor effect and is well tolerated in mice[1].

IC50 & Target：IAP[1] In Vitro Dasminapant (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells[1]. Dasminapant (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. Dasminapant sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Dasminapant Related Antibodies Western Blot Analysis[1] Cell Line: HepG2 and HCCLM3 cells

Hot selling product：α-Cyano-4-hydroxycinnamic acid  | ZT-12-037-01  | GSK503  | Ondansetron  | 680C91  | β-Carotene  | Mirzotamab  | Lobetyolin  | Pleconaril  | CellTracker CM-DiI

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References：

[1]. Chen Z, et, al. The SMAC Mimetic APG-1387 Sensitizes Immune-Mediated Cell Apoptosis in Hepatocellular Carcinoma. Front Pharmacol. 2018 Nov 6; 9:1298.  [Content Brief]

[2]. Li BX, et, al. Novel smac mimetic APG-1387 elicits ovarian cancer cell killing through TNF-alpha, Ripoptosome and autophagy mediated cell death pathway. J Exp Clin Cancer Res. 2018 Mar 12;37(1):53.  [Content Brief]

[3]. Li N, et, al. A novel Smac mimetic APG-1387 demonstrates potent antitumor activity in nasopharyngeal carcinoma cells by inducing apoptosis. Cancer Lett. 2016 Oct 10;381(1):14-22.  [Content Brief]

[4]. Li Q, et, al. Abstract 6216: Therapeutic potential of IAP inhibitor APG-1387 in combination with PARP- or MEK-targeted therapy, or chemotherapy in pancreatic cancer. American Association for Cancer Research. Aug 2020. 80(16).

[5]. Pan w, et, al. Abstract 1754: Smac mimetics APG-1387 synergizes with immune checkpoint inhibitors in preclinical models. American Association for Cancer Research. Jul 2018. 78(13).