AP 1903

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Cat.No. 6130 - AP 1903 | C78H98N4O20 | CAS No. 195514-63-7
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)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 141.16 100
ethanol 141.16 100

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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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References

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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