Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
ERα 5.08 μM (Ki) ERβ 26.20 μM (Ki)
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ln Vitro |
PROTAC ERα Degrader-4 (Compound ZD12) (1 μM, 12 hours) significantly degrades ERα in Tamoxifen-sensitive MCF-7 cells [1]. PROTAC ERα Degrader-4 (2 μM, 12 hours) can degrade wild-type ERα in T47D cells and mutant ERα in T47DD538G and T47DY537S cells [1]. PROTAC ERα Degrader-4 (1-10 μM, 72 hours) suppresses the development of Tamoxifen-sensitive MCF-7 cells with an IC50 value of 0.05 μM[1]. PROTAC ERα Degrader-4 (1-10 μM, 72 hours) causes apoptosis and cell cycle arrest in MCF-7 cells [1]. PROTAC ERα Degrader-4 (0.01-10 μM, 12 hours) significantly degrades ERα protein in MCF-7 cells [1].
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ln Vivo |
In the LCC2 xenograft tumor model, PROTAC ERα Degrader-4 (Compound ZD12) (5 μM/kg, intraperitoneal injection; once every two days) demonstrates strong anti-tumor effectiveness and ERα degradation activity [1]. The intravenous administration of 5 mg/kg of PROTAC ERα Degrader-4 resulted in a T1/2 of 4.61 hours and a clearance of 64.4 mL/min/kg [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: MCF-7 cells Tested Concentrations: 0.01-10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Had inhibitory activity in Tamoxifen-sensitive MCF-7 cells, with the IC50 value of 0.05 μM. Apoptosis Analysis[1] Cell Types: MCF-7 cells Tested Concentrations: 1.0 μM, 5 μM, 5.0 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced apoptosis. Cell Cycle Analysis[1] Cell Types: MCF-7 cells Tested Concentrations: 0.01-10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced cell cycle arrest. Western Blot Analysis[1] Cell Types: MCF-7 cells Tested Concentrations: 0.01-10 μM Incubation Duration: 12 hrs (hours) Experimental Results: Efficiently degraded ERα protein in the range of 0.01 to10 μM, whereas ERα protein levels recovered slightly at a high concentration of 10 μM |
References |
[1]. Xie B, et.al. Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer In Vitro and In Vivo. J Med Chem. 2023 May 25;66(10):6631-6651.
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Molecular Formula |
C55H62F3N5O10S2
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Molecular Weight |
1074.23
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CAS # |
2521299-80-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.9309 mL | 4.6545 mL | 9.3090 mL | |
5 mM | 0.1862 mL | 0.9309 mL | 1.8618 mL | |
10 mM | 0.0931 mL | 0.4654 mL | 0.9309 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.