AP1903

• CAT Number: I002495
• CAS Number: 195514-63-7
• Molecular Formula: C78H98N4O20
• Molecular Weight: 1411.63
• Purity: ≥95%
• Synonyms: AP1903; Rimiducid
• Target: Homodimerizers
• Solubility: DMSO: ≥ 54 mg/mL
• Storage: Store at -20°C
• IC50: 0.1 nM (EC50, HT1080)
• IUPAC Name: [(1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-[2-[[2-[3-[(1R)-3-(3,4-dimethoxyphenyl)-1-[(2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetyl]amino]ethylamino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate
• InChI: InChI=1S/C78H98N4O20/c1-13-57(53-43-67(93-7)73(97-11)68(44-53)94-8)75(85)81-37-17-15-25-59(81)77(87)101-61(31-27-49-29-33-63(89-3)65(39-49)91-5)51-21-19-23-55(41-51)99-47-71(83)79-35-36-80-72(84)48-100-56-24-20-22-52(42-56)62(32-28-50-30-34-64(90-4)66(40-
• InChIKey: GQLCLPLEEOUJQC-WFMNNBDOSA-N
• SMILES: O=C(NCCNC(COC1=CC([C@H](OC([C@H]2CCCCN2C([C@H](C3=CC(OC)=C(OC)C(OC)=C3)CC)=O)=O)CCC4=CC=C(OC)C(OC)=C4)=CC=C1)=O)COC5=CC([C@H](OC([C@H]6CCCCN6C([C@@H](CC)C7=CC(OC)=C(OC)C(OC)=C7)=O)=O)CCC8=CC=C(OC)C(OC)=C8)=CC=C5.

AP1903(CAT: I002495) is a synthetic compound that belongs to the class of macrolide antibiotics. It is important to note that AP1903 is also known as RAPAMYCIN-BINDING DOMAIN FUSION PROTEIN 1, or RAP1 for short. This is because AP1903 is not used as a drug on its own, but rather as a component of a gene therapy system. AP1903 is used to activate a fusion protein containing a rapamycin-binding domain and a protein of interest, allowing for controlled gene expression. This system is often used in research to study gene function and protein-protein interactions.

Reference

1:J Clin Pharmacol. 2001 Aug;41(8):870-9. Intravenous safety and pharmacokinetics of a novel dimerizer drug, AP1903, in healthy volunteers.Iuliucci JD,Oliver SD,Morley S,Ward C,Ward J,Dalgarno D,Clackson T,Berger HJ, PMID: 11504275
Abstract: AP1903 is a novel gene-targeted drug that is being developed for use in drug-regulated cell therapies. An intravenous, single-blind, placebo- and saline-controlled, ascending-dose study was performed to evaluate the safety, tolerability, and pharmacokinetics of AP1903. Twenty-eight normal healthy male volunteers were randomized into five dosage groups of AP1903 (0.01, 0.05, 0.1, 0.5, and 1 mg/kg). Within each group, 4 volunteers received a single dose of AP1903, 1 volunteer received an equal volume of placebo, and 1 received an equal volume of normal saline. The only exception was in the 0.5 mg/kg group, in which 4 volunteers were dosed: 3 received AP1903 and 1 received normal saline. All dosages were administered as intravenous infusions over 2 hours. Clinical safety parameters were monitored, and serial blood and urine samples were collected for analysis of AP1903. No drug-related adverse events were observed at any of the dose levels with the possible exception of facial flushing in 1 volunteer at the 1.0 mg/kg dose level. AP1903 plasma levels were directly proportional to the administered dose, with mean Cmax values ranging from approximately 10 to 1,275 ng/mL over the 0.01 to 1.0 mg/kg dose range. Following the infusion period, blood concentrations revealed a rapid distribution phase, with plasma levels being reduced to approximately 18%, 7%, and 1% of the maximal concentration at 0.5, 2, and 10 hours postdose, respectively. AP1903 was shown to be safe and well tolerated at all dose levels and demonstrated a favorable pharmacokinetic profile at doses well above the anticipated therapeutic dose.