| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PT-179 targets the E3 ubiquitin ligase cereblon (CRBN) as a selective molecular glue ligand. It is used in PROTAC applications to recruit CRBN for targeted protein degradation of proteins fused to a zinc finger degron.
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| ln Vitro |
SD40 is a degradation tag specific for PT-179. PT-179 (1-10 μM; 24 h) can induce eGFP degradation in HEK293T cells. The more evolved the degradation determinant variant is, the stronger the degradation efficiency of the corresponding tagged protein is[1].
PT-179 (1‑10 microM; 24 h) induces efficient degradation of eGFP in HEK293T cells when the target protein is fused to a zinc finger degron. Degradation potency increases with higher evolutionary optimization of the degron variant. |
| ln Vivo |
No in vivo activity data are specifically reported for PT-179 alone, as it is primarily used as a CRBN ligand in molecular glue or PROTAC constructs. In such constructs, it can mediate degradation of tagged proteins in animal models.
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| Enzyme Assay |
Binding affinity is measured by surface plasmon resonance (SPR) or fluorescence polarization (FP) assays using purified CRBN protein. PT‑179 is incubated with CRBN at graded concentrations, and the KD is calculated from saturation binding curves. A typical KD of 587 nM is reported.
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| Cell Assay |
HEK293T cells are transfected with plasmids expressing an eGFP‑ZF (zinc finger) fusion protein. Cells are treated with PT‑179 (1‑10 microM) for 24 h, then lysed and analyzed by Western blot or fluorescence microscopy to quantify eGFP degradation. Dose‑ and time‑dependent degradation is assessed.
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| Animal Protocol |
For a PROTAC construct containing PT‑179, mice bearing tumor xenografts expressing a target protein fused to a ZF degron are treated orally or intraperitoneally with the compound. Tumor tissue is collected post‑treatment and analyzed for target protein levels by Western blot or immunohistochemistry.
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| ADME/Pharmacokinetics |
PT‑179 is soluble in DMSO at 100 mg/mL. For in vitro use, stock solutions are stored at ‑20degC for up to 1 month. For in vivo formulations, it can be dissolved in 10% DMSO / 40% PEG300 / 5% Tween‑80 / 45% saline or 10% DMSO / 90% corn oil. No detailed PK parameters are available.
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| Toxicity/Toxicokinetics |
PT‑179 has greatly reduced off‑target degradation activity compared to pomalidomide, as it does not induce degradation of known pomalidomide neosubstrates. The compound is not for human use; general safety precautions for laboratory handling apply.
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| References | |
| Additional Infomation |
PT‑179 is an orthogonal thalidomide derivative developed for selective CRBN targeting with minimized off‑target effects. It serves as a valuable tool for studying molecular glue mechanisms and for constructing zinc‑finger‑based PROTAC degraders. The compound is for research use only and has not entered clinical trials or received marketing approval.
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| Molecular Formula |
C17H17N3O5
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|---|---|
| Molecular Weight |
343.33
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| Exact Mass |
343.116
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| CAS # |
2924858-25-1
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| PubChem CID |
163294079
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| Appearance |
Solid powder
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| Density |
1.460±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
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| Boiling Point |
643.7±55.0 °C(predicted)
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| LogP |
0.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
615
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C2=CC(N3CCOCC3)=CC=C2C(N1C1CCC(NC1=O)=O)=O
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| InChi Key |
CCCSRHUSXCBFJZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17N3O5/c21-14-4-3-13(15(22)18-14)20-16(23)11-2-1-10(9-12(11)17(20)24)19-5-7-25-8-6-19/h1-2,9,13H,3-8H2,(H,18,21,22)
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| Chemical Name |
2-(2,6-dioxopiperidin-3-yl)-5-morpholin-4-ylisoindole-1,3-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 125 mg/mL (364.08 mM; with sonication (<60°C))
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9126 mL | 14.5632 mL | 29.1265 mL | |
| 5 mM | 0.5825 mL | 2.9126 mL | 5.8253 mL | |
| 10 mM | 0.2913 mL | 1.4563 mL | 2.9126 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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