APG-1387

• CAT Number: I022312
• CAS Number: 1570231-89-8
• Molecular Formula: C60H72N10O10S2
• Molecular Weight: 1157.42
• Purity: ≥95%
• Solubility: Soluble in DMSO, not in water
• Storage: Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
• IUPAC Name: (5S,5'S,8S,8'S,10aR,10a'R)-3,3'-(1,3-phenylenedisulfonyl)bis(N-benzhydryl-5-((S)-2-(methylamino)propanamido)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide)
• InChI: InChI=1S/C60H72N10O10S2/c1-39(61-3)55(71)63-49-37-67(34-32-45-28-30-51(69(45)59(49)75)57(73)65-53(41-18-9-5-10-19-41)42-20-11-6-12-21-42)81(77,78)47-26-17-27-48(36-47)82(79,80)68-35-33-46-29-31-52(70(46)60(76)50(38-68)64-56(72)40(2)62-4)58(74)66-54(43-22-13-7-14-23-43)44-24-15-8-16-25-44/h5-27,36,39-40,45-46,49-54,61-62H,28-35,37-38H2,1-4H3,(H,63,71)(H,64,72)(H,65,73)(H,66,74)/t39-,40-,45+,46+,49-,50-,51-,52-/m0/s1
• InChIKey: AKLBERUGKZNEJY-RTEPGWBGSA-N
• SMILES: O=C(NC(C1=CC=CC=C1)C2=CC=CC=C2)[C@@H]3CC[C@H](CCN(S(C4=CC=CC(S(N(C[C@@H]5NC([C@H](C)NC)=O)CC[C@@H]6N([C@H](C(NC(C7=CC=CC=C7)C8=CC=CC=C8)=O)CC6)C5=O)(=O)=O)=C4)(=O)=O)C[C@@H]9NC([C@@H](NC)C)=O)N3C9=O

APG-1387 (Cat.No:I022312), also known as SM-1387, is a IAP inhibitor. APG-1387 promotes the rapid degradation of cIAP1/2 and XIAP, and it exerts an antitumor effect on nasopharyngeal carcinoma cancer stem cells. Further studies show that APG-1387 enhances the chemosensitivity and promotes apoptosis in combination with CDDP and 5-FU of NPC in vitro and vivo.

Reference

1: Rzymski T, Mikula M, Żyłkiewicz E, Dreas A, Wiklik K, Gołas A, Wójcik K, Masiejczyk M, Wróbel A, Dolata I, Kitlińska A, Statkiewicz M, Kuklinska U, Goryca K, Sapała Ł, Grochowska A, Cabaj A, Szajewska-Skuta M, Gabor-Worwa E, Kucwaj K, Białas A, Radzimierski A, Combik M, Woyciechowski J, Mikulski M, Windak R, Ostrowski J, Brzózka K. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795. doi: 10.18632/oncotarget.16810. PubMed PMID: 28422713; PubMed Central PMCID: PMC5464911.
2: Li N, Feng L, Han HQ, Yuan J, Qi XK, Lian YF, Kuang BH, Zhang YC, Deng CC, Zhang HJ, Yao YY, Xu M, He GP, Zhao BC, Gao L, Feng QS, Chen LZ, Yang L, Yang D, Zeng YX. 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. Epub 2016 Jul 15. PubMed
PMID: 27424523.