APG-1387

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). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.

Product information

CAS Number: 1570231-89-8

Molecular Weight: 1157.40

Formula: C60H72N10O10S2

Chemical Name: (5S,8S,10aR)-3-(3-{[(5S,8S,10aR)-8-[(diphenylmethyl)carbamoyl]-5-[(2S)-2-(methylamino)propanamido]-6-oxo-decahydropyrrolo[1,2-a][1,5]diazocin-3-yl]sulfonyl}benzenesulfonyl)-N-(diphenylmethyl)-5-[(2S)-2-(methylamino)propanamido]-6-oxo-decahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide

Smiles: C[C@H](NC)C(=O)N[C@H]1CN(CC[C@H]2CC[C@@H](C(=O)NC(C3C=CC=CC=3)C3C=CC=CC=3)N2C1=O)S(=O)(=O)C1C=C(C=CC=1)S(=O)(=O)N1C[C@H](NC(=O)[C@H](C)NC)C(=O)N2[C@@H](CC[C@@H]2CC1)C(=O)NC(C1C=CC=CC=1)C1C=CC=CC=1

InChiKey: AKLBERUGKZNEJY-RTEPGWBGSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (43.20 mM; Need ultrasonic). H2O : < 0.1 mg/mL (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

APG-1387 (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells. APG-1387 (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. APG-1387 sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro.

In Vivo:

APG-1387 (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice. APG-1387 (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.

Products are for research use only. Not for human use.