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Description: Chemical inducer of protein dimerization; active in vivo
Chemical Name: 2,2'-[1,2-Ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] bis[(2S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate]
Purity: ≥98% (HPLC)
Biological Activity for AP 1903
AP 1903 is a chemical protein dimerizer for use in FKBP fusion protein systems. Induces apoptosis in cells expressing a fusion protein consisting of FKBPF36V and intracellular domain of Fas receptor with high potency (EC50 = 0.1 nM). Exhibits >50-fold selectivity for FKBPF36V-Fas fusion protein over wild-type FKBP. Also induces apoptosis in cells expressing Cas9-FK506 fusion proteins, in inducible caspase 9 (iCas9) suicide gene system. Active in vivo.
Technical Data for AP 1903
| M. Wt | 1411.65 |
| Formula | C78H98N4O20 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 195514-63-7 |
| PubChem ID | 16135625 |
| InChI Key | GQLCLPLEEOUJQC-ZTQDTCGGSA-N |
| Smiles | O=C([C@@H]1CCCCN1C([C@H](C2=CC(OC)=C(OC)C(OC)=C2)CC)=O)O[C@@H](C3=CC(OCC(NCCNC(COC4=CC=CC([C@H](OC([C@@H]5CCCCN5C([C@H](C6=CC(OC)=C(OC)C(OC)=C6)CC)=O)=O)CCC7=CC(OC)=C(OC)C=C7)=C4)=O)=O)=CC=C3)CCC8=CC(OC)=C(OC)C=C8 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AP 1903
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 141.16 | 100 | |
| ethanol | 141.16 | 100 |
Preparing Stock Solutions for AP 1903
The following data is based on the product molecular weight 1411.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.71 mL | 3.54 mL | 7.08 mL |
| 5 mM | 0.14 mL | 0.71 mL | 1.42 mL |
| 10 mM | 0.07 mL | 0.35 mL | 0.71 mL |
| 50 mM | 0.01 mL | 0.07 mL | 0.14 mL |
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Product Datasheets for AP 1903
References for AP 1903
References are publications that support the biological activity of the product.
Clackson et al (1998) Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc.Natl.Acad.Sci.USA. 95 10437 PMID: 9724721
Gargett & Brown (2014) The inducible caspase-9 suicide gene system as a "safety switch" to limit on-target, off-tumor toxicities of chimeric antigen receptor T cells. Front.Pharmacol. 5 235 PMID: 25389405
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Keywords: AP 1903, AP 1903 supplier, AP1903, Chemical, protein, dimerizer, iCas9, inducible, caspase, 9, suicide, gene, induces, inducers, apoptosis, FKBPF36V, fusion, FK506-binding, Protein, Dimerizers, 6130, Tocris Bioscience
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