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  • DC Chemicals Limited
  • China
  • Product Name: AP1903
  • Price: $950.0/100mg $1850.0/250mg $3750.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

195514-63-7

195514-63-7 structure
195514-63-7 structure
  • Name: AP 1903
  • Chemical Name: AP1903
  • CAS Number: 195514-63-7
  • Molecular Formula: C78H98N4O20
  • Molecular Weight: 1411.627
  • Catalog: Signaling Pathways Apoptosis TNF Receptor
  • Create Date: 2018-10-17 21:14:47
  • Modify Date: 2024-01-04 20:26:50
  • Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains, initiating Fas signaling and hence apoptosis.

Name AP1903
Synonyms AP1903
AP-1903
UNII:H564L1W5J2
H564L1W5J2
Rimiducid
2-piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, 1,2-ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene(1R)-3-(3,4-dimethoxyphenyl)propylidene] ester, (2S,2'S)-
ethane-1,2-diylbis[imino(2-oxoethane-2,1-diyl)oxybenzene-3,1-diyl(1R)-3-(3,4-dimethoxyphenyl)propane-1,1-diyl] (2S,2'S)bis{1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate}
1,2-Ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene(1R)-3-(3,4-dimethoxyphenyl)-1,1-propanediyl] (2S,2'S)bis{1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]-2-piperidinecarboxylate}
Description Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains, initiating Fas signaling and hence apoptosis.
Related Catalog
Target

EC50: 0.1 nM (FKBP, in HT1080 cells)[1] Fas receptor[1]

In Vitro The human fibrosarcoma line HT1080 is engineered to express stably a fusion protein comprising a myristoylation sequence, two copies of F36V-FKBP, and the human first apoptosis signal (Fas) intracellular domain. Rimiducid (AP1903) elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC50 of ≈0.1 nM[1]. Maximal killing occurred in the presence of 3 to 10 nM Rimiducid (AP1903), and the IC50 is approximately 0.2 nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after Rimiducid treatment[2].
In Vivo Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum hGH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg[1].
Cell Assay Cloned HT1080 cell lines (ATCC CCL-121) retrovirally transduced with Fas constructs are prepared. Cell viability after overnight incubation with Rimiducid (0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM) is measured by Alamar Blue assay[1]. For annexin V assays, sorted LV′VFas-transduced T cells (2×106 cells/mL) are incubated with 10 nM Rimiducid. At the indicated time, an aliquot of 2×105 cells is taken, stained with annexin V-fluorescein isothiocyanate, and analyzed by flow cytometry[2].
Animal Admin Mice[1] Male nu/nu mice are used. For injection, HTFasGH-3 cells are harvested from tissue culture dishes in PBS/0.1% glucose/10 mM EDTA, washed, and resuspended in PBS/0.1% BSA/0.1% glucose at a concentration of 2×107 cells/mL. Between 2 and 4×106 cells are implanted into two i.m. sites. After 24 h, mice are administered i.v. Rimiducid at 2 mL/kg. After a further 24 h mice are killed and serum hGH concentrations are determined by ELISA.
References

[1]. Clackson T, et al. Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42.

[2]. Thomis DC, et al. A Fas-based suicide switch in human T cells for the treatment of graft-versus-host disease. Blood. 2001 Mar 1;97(5):1249-57.

[3]. Valamehr, Bahram, et al. GENOMIC ENGINEERING OF PLURIPOTENT CELLS. Patent. US20180155717A1.

Density 1.2±0.1 g/cm3
Boiling Point 1307.5±65.0 °C at 760 mmHg
Molecular Formula C78H98N4O20
Molecular Weight 1411.627
Flash Point 744.5±34.3 °C
Exact Mass 1410.677490
LogP 10.39
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.566
Storage condition 2-8℃