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AP20187 (Synonyms: B/B Homodimerizer)

Catalog No.GC14498

Dimerizer,synthetic and cell-permeable

Products are for research use only. Not for human use. We do not sell to patients.

AP20187 Chemical Structure

Cas No.: 195514-80-8

Size Price Stock Qty
1mg
$87.00
In stock
10mg
$344.00
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5mg
$216.00
In stock
10mM (in 1mL DMSO)
$561.00
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50mg
$1,040.00
In stock
25mg
$672.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment: [1]

Cell lines

CHO-AA8-Tet off cells

Preparation method

The solubility of this compound in DMSO is >74.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

Applications

The cDNAs for the MLL-AF9 fusion protein were transfected in triplicate into CHO cells along with a Myc E box HSV TK luciferase reporter and a CMV-driven Renilla luciferase control plasmid. Results are expressed as a ratio of normalized firefly luciferase activity to the activity of cells transfected with an MSCV neomycin control vector. In the presence of the dimerizer AP20187, cells transfected with MLL-FKBP showed strong dose-dependent transactivation of the Myc E box HSV TK reporter. The dimerization of the fusion protein activated transcription with nearly 250-fold.

Animal experiment: [2]

Animal models

CD1 mice

Dosage form

Intraperitoneal injection, 10 mg/kg

Applications

To evaluate LFv2IRE expression and tyrosine phosphorylation, CD1 mice were injected via the tail vein with GC of AAV2/8-TBG-LFv2IRE or AAV2/1-MCK-LFv2IRE vector 4 weeks before the AP20187 injection. AP20187-dependent LFv2IRE tyrosine phosphorylation was evident 2 hr after drug administration, peaked 6 hr later, and returned to baseline after 24 hr. Low LFv2IRE basal phosphorylation was detected in liver samples from mice receiving AAV2/8-TBG-LFv2IRE but not stimulated with AP20187, suggesting minimal leakiness of the system.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Martin M E, Milne T A, Bloyer S, et al. Dimerization of MLL fusion proteins immortalizes hematopoietic cells. Cancer cell, 2003, 4(3): 197-207.

[2] Cotugno G, Formisano P, Giacco F, et al. AP20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice. Human gene therapy, 2007, 18(2): 106-117.

Background

AP20187 is a small dimerizer drug [1].

To solve the graft-versus-host disease, the in vivo behavior of the transplanted cells should be controlled. AP20187 is used in the conditional system as a chemical inducer of dimerization (CID). Another component is a fusion protein. The CIDs have advantages in gene therapy, it offers the possibility of achieving selection without the toxic effects. In vivo studies show that AP20187 can produces a notable expansion of transduced red cells, platelets, and to a lesser extent, granulocytes [1].

AP20187 is also reported to be used in an AP20187–LFv2IRE system. In this system, AP20187 administration causes the activation of LFv2IRE and results in increased uptake of both hepatic glycogen content and muscular glucose [2].

References:
[1] Neff T, Blau CA. Pharmacologically regulated cell therapy. Blood. 2001 May 1;97(9):2535-40.
[2] Cotugno G, Formisano P, Giacco F, Colella P, Beguinot F, Auricchio A. AP20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice. Hum Gene Ther. 2007 Feb;18(2):106-17.

Chemical Properties

Cas No. 195514-80-8 SDF
Synonyms B/B Homodimerizer
Canonical SMILES O=C([C@@H]1CCCCN1C([C@@H](CC)C2=CC(OC)=C(OC)C(OC)=C2)=O)O[C@H](CCC3=CC(OC)=C(OC)C=C3)C4=CC=CC(OCC(NCC(CNC(COC5=CC=CC([C@@H](CCC6=CC(OC)=C(OC)C=C6)OC([C@H]7N(C([C@@H](CC)C8=CC(OC)=C(OC)C(OC)=C8)=O)CCCC7)=O)=C5)=O)CN(C)C)=O)=C4
Formula C82H107N5O20 M.Wt 1482.75
Solubility ≥ 74.1375mg/mL in DMSO, ≥ 50mg/ml in 75% ethanol aqueous solution Storage Store at -20°C,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 0.6744 mL 3.3721 mL 6.7442 mL
5 mM 0.1349 mL 0.6744 mL 1.3488 mL
10 mM 0.0674 mL 0.3372 mL 0.6744 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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