AP 1867

Pricing Availability   Qty
Description: Selective binding ligand for FKBP12F36V
Chemical Name: (1R)-1-[3-(Carboxymethoxy)phenyl]-3-(3,4-dimethoxyphenyl)propyl (2S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity for AP 1867

AP 1867 is a selective binding ligand for the single point mutant of FKBP12F36V (IC50 = 1.8 nM). Functionalized with a carboxylic acid group at the meta-position to enable onward chemistry. The position of the carboxylic acid group represents an 'exit vector' allowing modification without interfering with the compound's binding ability.

Technical Data for AP 1867

M. Wt 693.79
Formula C38H47NO11
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 195514-23-9
PubChem ID 444590
InChI Key XCCRAOPQCACRFC-OIFRRMEBSA-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(O)=O)=CC=C3)CCC4=CC(OC)=C(OC)C=C4

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 1867

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 69.38 100
DMSO 69.38 100

Preparing Stock Solutions for AP 1867

The following data is based on the product molecular weight 693.79. 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 1.44 mL 7.21 mL 14.41 mL
5 mM 0.29 mL 1.44 mL 2.88 mL
10 mM 0.14 mL 0.72 mL 1.44 mL
50 mM 0.03 mL 0.14 mL 0.29 mL

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References for AP 1867

References are publications that support the biological activity of the product.

Koide et al (2001) A synthetic library of cell-permeable molecules. J.Am.Chem.Soc. 123 398 PMID: 11456541

Clackson et al (1998) Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc.Natl.Acad.Sci.U.S.A. 95 10437 PMID: 9724721


If you know of a relevant reference for AP 1867, please let us know.

Keywords: AP 1867, AP 1867 supplier, AP1867, dTAG, FKBP, FK506, building, block, chemical, biology, FKBP12, FKBP12F36V, onward, chemistry, carboxylic, acid, group, TAG, Degradation, Platform, 6207, Tocris Bioscience

Citations for AP 1867

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Targeted Protein Degradation Research Product Guide

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The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple WesternTM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.