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| Product Name: | AP1903 | | Synonyms: | AP1903;Rimiducid(AP1903);AP1903;RIMIDUCID;AP-1903;AP1903
(Rimiducid;CS-1237;RIMIDUCID;AP-1903;AP 1903;2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, 2,2'-[1,2-ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] ester, (2S,2'S)-;(1R,1'R)-((((Ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate) | | CAS: | 195514-63-7 | | MF: | C78H98N4O20 | | MW: | 1411.63 | | EINECS: | 604-604-1 | | Product Categories: | | | Mol File: | 195514-63-7.mol |  |
| | AP1903 Chemical Properties |
| Boiling point | 1307.5±65.0 °C(Predicted) | | density | 1?+-.0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO:97.05(Max Conc. mg/mL);68.75(Max Conc. mM)
Ethanol:120.58(Max Conc. mg/mL);85.42(Max Conc. mM) | | form | A solid | | pka | 13.70±0.46(Predicted) | | color | White to light yellow |
| | AP1903 Usage And Synthesis |
| Biological Activity | AP1903 (Rimiducid) is a dimerizing agent that acts by cross-linking the FKBP domain, initiating Fas signaling and causing apoptosis.It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis. | | 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 EC 50 of ≈0.1 nM. Maximal killing occurred in the presence of 3 to 10 nM Rimiducid (AP1903), and the IC 50 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. | | in vivo | AP1903 elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg /kg. | | target | EC50: 0.1 nM (FKBP, in HT1080 cells)
Fas receptor | | storage | Store at -20°C |
| | AP1903 Preparation Products And Raw materials |
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