| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DEG-77 targets the zinc finger transcription factor IKZF2 (Aiolos) and the serine/threonine protein kinase CK1α (casein kinase 1 alpha). As a molecular glue degrader, DEG-77 works by co-opting the E3 ubiquitin ligase Cereblon (CRBN) to induce proximity between CRBN and its neo-substrates, leading to their ubiquitination and subsequent degradation by the proteasome. IKZF2 is a transcription factor involved in lymphocyte development and immune regulation, while CK1α is a kinase that plays roles in Wnt signaling and cell cycle regulation.
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| ln Vitro |
As a molecular glue degrader, DEG-77 shows potent in vitro degradation activity with DC50 values of 15.3 nM for IKZF2 and 10 nM for CK1α. The compound induces selective degradation of its target proteins through the ubiquitin-proteasome pathway. This degradation mechanism enables the compound to eliminate target proteins rather than merely inhibiting their activity. DEG-77 can be used for acute myeloid leukemia (AML) study.
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| ln Vivo |
In vivo activity of DEG-77 has been suggested based on its suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies. The compound has a half-life of 8 hours, supporting its use in animal models. DEG-77's ability to degrade IKZF2 and CK1α in vivo positions it as a promising tool for studying the role of these proteins in hematological malignancies and other diseases.
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| Enzyme Assay |
Non-cell-based binding assays for DEG-77 typically involve measuring the affinity of the compound for Cereblon (CRBN) and its neo-substrates (IKZF2 and CK1α). A standard protocol includes surface plasmon resonance (SPR) or fluorescence polarization (FP) using purified CRBN protein and target proteins. The compound's ability to induce ternary complex formation between CRBN and its neo-substrates can be assessed using biochemical binding assays. The degradation activity is typically evaluated in cell-based systems.
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| Cell Assay |
Cellular assays for DEG-77 typically involve acute myeloid leukemia cell lines or other cell lines dependent on IKZF2 or CK1α. A representative protocol includes: culturing cells in appropriate medium, treating with DEG-77 at various concentrations (0.001–1000 nM) for 4–24 hours, and measuring target protein levels (IKZF2 and CK1α) by Western blot to determine the DC50 (half-maximal degradation concentration). Cell viability is assessed using CellTiter-Glo assays to evaluate antiproliferative effects.
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| Animal Protocol |
In vivo animal studies with DEG-77 are conducted in xenograft mouse models of acute myeloid leukemia or other cancers dependent on IKZF2 or CK1α. A typical protocol involves subcutaneous implantation of tumor cells in immunodeficient mice, allowing tumors to reach a certain size, administering DEG-77 via oral gavage or intraperitoneal injection at doses determined from pharmacokinetic studies (t1/2=8h), monitoring tumor growth and body weight, and harvesting tumors for analysis of target protein degradation by Western blot.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DEG-77 have been characterized for in vivo studies. The compound has a half-life of 8 hours. DEG-77 has a molecular weight of 447.44 g/mol and a molecular formula of C24H21N3O6. Solubility: DMSO at 50 mg/mL (111.75 mM; with sonication <80°C). In vivo formulation: 10% DMSO + 90% Corn Oil (solubility: 2.5 mg/mL, 5.59 mM). Storage: Powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month.
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| Toxicity/Toxicokinetics |
As a research compound, DEG-77 is not intended for human therapeutic use, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening, hERG channel inhibition testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity. The compound is for research use only.
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| References | |
| Additional Infomation |
DEG-77 (CAS 3032265-06-5) is a targeted molecular glue that induces the degradation of IKZF2 and CK1α with DC50 values of 15.3 nM and 10 nM, respectively. The compound possesses suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies (t1/2=8h). DEG-77 can be used for acute myeloid leukemia (AML) study. The compound is referenced in the primary literature for its degradation activity and represents a promising approach for targeting IKZF2 and CK1α in cancer research.
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| CAS # |
3032265-06-5
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| Appearance |
Light yellow to green yellow solid powder
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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 :~50 mg/mL (~111.75 mM; with sonication (<80°C))
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.59 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
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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