AP1903
- Product Name
- AP1903
- CAS No.
- 195514-63-7
- Chemical Name
- AP1903
- 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)-;(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);(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);(S,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) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
- CBNumber
- CB92627330
- Molecular Formula
- C78H98N4O20
- Formula Weight
- 1411.63
- MOL File
- 195514-63-7.mol
AP1903 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 6130
- Product name
- AP1903
- Purity
- ≥98%(HPLC)
- Packaging
- 5
- Price
- $335
- Updated
- 2021/12/16
- Product number
- B4168
- Product name
- AP1903
- Packaging
- 50mg
- Price
- $1425
- Updated
- 2021/12/16
- Product number
- CS-3162
- Product name
- Rimiducid
- Purity
- 99.81%
- Packaging
- 50mg
- Price
- $1680
- Updated
- 2021/12/16
- Product number
- B4168
- Product name
- AP1903
- Packaging
- 100mg
- Price
- $1995
- Updated
- 2021/12/16
- Product number
- CS-3162
- Product name
- Rimiducid
- Purity
- 99.81%
- Packaging
- 100mg
- Price
- $2280
- Updated
- 2021/12/16
AP1903 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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