| Identification | Back Directory | [Name]
APG-1387 | [CAS]
1570231-89-8 | [Synonyms]
SM1387
SM-1387
SM 1387
APG-1387
APG 1387l
Pyrrolo[1,2-a][1,5]diazocine-8-carboxamide, 3,3'-[1,3-phenylenebis(sulfonyl)]bis[N-(diphenylmethyl)decahydro-5-[[(2S)-2-(methylamino)-1-oxopropyl]amino]-6-oxo-, (5S,5'S,8S,8'S,10aR,10'aR)-
(5S,8S,10aR)-N-benzhydryl-3-((3-(((5R,8S,10aS)-8-(benzhydrylcarbamoyl)-5-((S)-2-(methylamino)propanamido)-6-oxooctahydropyrrolo[1,2-a][1,5]diazocin-3(4H)-yl)sulfonyl)phenyl)sulfonyl)-5-((S)-2-(methylamino)propanamido)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide | [Molecular Formula]
C60H72N10O10S2 | [MDL Number]
MFCD32878242 | [MOL File]
1570231-89-8.mol | [Molecular Weight]
1157.4 |
| Chemical Properties | Back Directory | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, stored under nitrogen | [solubility ]
DMSO : 50 mg/mL (43.20 mM; Need ultrasonic)| | [form ]
Solid | [pka]
13.17±0.40(Predicted) | [color ]
White to off-white | [Water Solubility ]
Water : < 0.1 mg/mL (insoluble) |
| Hazard Information | Back Directory | [Uses]
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[1][2][3][4][5]. | [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]. | Animal Model: | Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells[1] | | Dosage: | 20 mg/kg | | Administration: | I.p. every 3 days for 4 weeks | | Result: | Decreased the expression of cIAP1 and cIAP2, and less potent to XIAP expression.
Potentiated the effects of pre-activated NK cells on HCCLM3 xenograft tumor growth and tumor weight.
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| [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. DOI:10.3389/fphar.2018.01298
[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. DOI:10.1186/s13046-018-0703-9
[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. DOI:10.1016/j.canlet.2016.07.008
[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). |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|