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.
Cas No.: 195514-80-8
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment: [1] | |
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Cell lines |
CHO-AA8-Tet off cells |
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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. |
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Reaction Conditions |
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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] | |
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Animal models |
CD1 mice |
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Dosage form |
Intraperitoneal injection, 10 mg/kg |
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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. |
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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. |
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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. |
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| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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