| Identification | Back Directory | [Name]
AP1903 | [CAS]
195514-63-7 | [Synonyms]
AP1903
CS-1237
Rimiducid(AP1903)
AP1903
(Rimiducid
AP1903;RIMIDUCID;AP-1903
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)- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C78H98N4O20 | [MDL Number]
MFCD25976784 | [MOL File]
195514-63-7.mol | [Molecular Weight]
1411.63 |
| Chemical Properties | Back Directory | [Boiling point ]
1307.5±65.0 °C(Predicted) | [density ]
1?+-.0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,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 |
| Hazard Information | Back Directory | [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 |
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