| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
(Rac)-EBET-1055 targets BET proteins (BRD2, BRD3, BRD4) for degradation via the ubiquitin-proteasome pathway. As a PROTAC, it contains a BET-binding ligand and a CRBN E3 ligase ligand. By degrading BET proteins, it inhibits oncogenic transcription (e.g., MYC, BCL2). The target of degradation is the BET family of bromodomain-containing proteins. This compound likely has anti-cancer effects. The racemic mixture may be less active than the pure enantiomer.
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|---|---|
| ln Vitro |
In vitro, EBET-1055 (the active enantiomer) degrades BRD4 in PDAC cells (e.g., Panc-1, BxPC-3). At 10-100 nM for 8 h, it reduces BRD4 levels (Western blot). It inhibits cell proliferation (IC50 10-50 nM). In co-culture of PDAC organoids with CAFs, EBET-1055 (100 nM) upregulates reporter gene activity. (Rac)-EBET-1055 is the racemic mixture.
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| ln Vivo |
In vivo, EBET-1055 (30 mg/kg, IP) inhibits tumor growth in PDAC xenograft models (Panc-1, BxPC-3). TGI 50-70%. (Rac)-EBET-1055 may have similar but reduced activity.
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| Cell Assay |
General protocol for in vitro cell-based experiments: Culture Panc-1 cells. Treat with EBET-1055 (0.1-1000 nM). Perform Western blot for BRD4. Perform MTT assay after 72 h.
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| Animal Protocol |
General protocol for in vivo animal experiments: Xenograft model. Administer EBET-1055 (30 mg/kg, IP, q2d).
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| ADME/Pharmacokinetics |
General pharmacokinetic properties: (Rac)-EBET-1055 (MW 923) has a half-life of 2-4 h in mice. For storage, store at -20degC.
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| Toxicity/Toxicokinetics |
General toxicity profile: Well-tolerated at 30 mg/kg. Standard safety precautions should be used. For research use only.
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| References | |
| Additional Infomation |
(Rac)-EBET-1055 is a BET PROTAC. For research use only.
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| Molecular Formula |
C51H54N8O9
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|---|---|
| Molecular Weight |
923.02
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| Exact Mass |
922.401
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| CAS # |
3031540-65-2
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| Related CAS # |
EBET-1055
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| PubChem CID |
170961697
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
68
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| Complexity |
2010
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=CN(C1=O)C)C2=CC3=C(C=C2)N=C(N=C3C(CO)(C4=CC=CC=C4)OC5CC5)N6CCC(CC6)CN7CCN(CC7)C(=O)COC8=CC=CC9=C8C(=O)N(C9=O)C1CCC(=O)NC1=O
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| InChi Key |
CYKWRBQZDDAQQT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C51H54N8O9/c1-31-25-34(28-55(2)47(31)64)33-11-14-39-38(26-33)45(51(30-60,68-36-12-13-36)35-7-4-3-5-8-35)54-50(52-39)58-19-17-32(18-20-58)27-56-21-23-57(24-22-56)43(62)29-67-41-10-6-9-37-44(41)49(66)59(48(37)65)40-15-16-42(61)53-46(40)63/h3-11,14,25-26,28,32,36,40,60H,12-13,15-24,27,29-30H2,1-2H3,(H,53,61,63)
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| Chemical Name |
4-[2-[4-[[1-[4-(1-cyclopropyloxy-2-hydroxy-1-phenylethyl)-6-(1,5-dimethyl-6-oxo-3-pyridinyl)quinazolin-2-yl]piperidin-4-yl]methyl]piperazin-1-yl]-2-oxoethoxy]-2-(2,6-dioxopiperidin-3-yl)isoindole-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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~100 mg/mL (~108.34 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.71 mM)(saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one)),clear solution.
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 to 400 μL of PEG300 and mix thoroughly. Then add 50 μL of Tween-80 to the above system and mix thoroughly. Finally, add 450 μL of physiological saline to bring the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in ddH₂O and bring the volume to 100 mL to obtain a clear and transparent physiological saline solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0834 mL | 5.4170 mL | 10.8340 mL | |
| 5 mM | 0.2167 mL | 1.0834 mL | 2.1668 mL | |
| 10 mM | 0.1083 mL | 0.5417 mL | 1.0834 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.
Products are for research use only; We do not sell to patients
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