APG-1387 - ≥99% , CAS No.1570231-89-8

CAS: 1570231-89-8 Cat. No.: A647711 Molecular Weight: 1157.40 PubChem CID: 73336238

GRADE & PURITY ≥99%

Storage

Store at -20°C,Argon charged

Shipped In

Ice chest + Ice pads

Overview

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

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HepG2 and HCCLM3 cells Concentration: 0.02, 0.2, 2, 20 μM Incubation Time: 1, 6, 24 hours Result: Decreased the expression of cIAP1 and cIAP2 in both cell lines in a dose- and time-dependent manner. Inhibited the expression of X chromosome-linked IAP (XIAP) at a high dose.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells 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.

Form:Solid

IC50& Target:IAP

Specifications

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

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 l

Storage

Store at -20°C, Argon charged

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ANTAGONIST

Purity

≥99%

Names and Identifiers

• Isomeric SMILES: C[C@@H](C(=O)N[C@H]1CN(CC[C@H]2CC[C@H](N2C1=O)C(=O)NC(C3=CC=CC=C3)C4=CC=CC=C4)S(=O)(=O)C5=CC(=CC=C5)S(=O)(=O)N6CC[C@H]7CC[C@H](N7C(=O)[C@H](C6)NC(=O)[C@H](C)NC)C(=O)NC(C8=CC=CC=C8)C9=CC=CC=C9)NC
• PubChem CID: 73336238
• Molecular Weight: 1157.40

Chemical and Physical Properties

• Solubility: DMSO : 50 mg/mL (43.20 mM; Need ultrasonic) H2O : <0.1 mg/mL (insoluble)
• Molecular Weight: 1157.400 g/mol
• XLogP3: 4.500
• Hydrogen Bond Donor Count: 6
• Hydrogen Bond Acceptor Count: 14
• Rotatable Bond Count: 18
• Exact Mass: 1156.49 Da
• Monoisotopic Mass: 1156.49 Da
• Topological Polar Surface Area: 273.000 Ų
• Heavy Atom Count: 82
• Formal Charge: 0
• Complexity: 2240.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 8
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 1