MC-Val-Cit-PAB-PROTAC ERα Degrader-1
Based on 1 Customer Validation
MC-Val-Cit-PAB-PROTAC ERα Degrader-1 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. MC-Val-Cit-PAB-PROTAC ERα Degrader-1 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
For research use only. We do not sell to patients.
- Purity: 99.18%
- CAS No.: 2158322-33-7
- Formula: C94H107N13O16
- Molecular Weight:1674.93
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Estrogen receptor-alpha (ERα)[1]
Treatment of HER2 expressing cells with HER2 antibody containing PAC Anti-HER2(Endox-XIAP) results in a marked decreased Estrogen Receptor-alpha (ERα) levels with an IC50 of 132 ng/mL. The PROTAC-Antibody Conjugate (PAC) molecules comprise an antibody conjugated via a linker (L1) to a PROTAC, wherein the PROTAC comprises an ubiquitin E3 ligase binding group ( "E3LB" ), a linker ( "L2" ) and a protein binding group ( "PB" ). The following sections describe the components that comprise the PAC. To obtain a PAC having potent efficacy and a desirable therapeutic index, the following components are provided. 1. Antibody (Ab): The antibody portion of a PAC can target a cell that expresses an antigen whereby the antigen specific PAC is delivered intracellularly to the target cell, typically through endocytosis While PACs that comprise an antibody directed to an antigen that is not found on the cell surface may result in less specific intracellular delivery of the PROTAC portion into the cell, the PAC may still undergo pinocytosis. 2. Linkers (L1): A "linker" (L1) is a bifunctional or multifunctional moiety that can be used to link one or more PROTAC moieties (D) to an antibody (Ab) to form a PAC. In some embodiments, PACs can be prepared using a L1 having reactive functionalities for covalently attaching to the PROTAC and to the antibody. 3. PROTAC(D) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2158322-33-7
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Appearance Solid
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Molecular Weight 1674.93
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Formula C94H107N13O16
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Color White to off-white
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SMILES
CN(C(COCCOCCNC(C1=CC=C(C(N2[C@@H](C)[C@H](NC([C@H](C)NC)=O)C(N(CC3=C(OC)C=CC4=C3C=CC=C4)C5=C2C=C(C#N)C=C5)=O)=O)C=C1)=O)=O)CCOC(C=C6)=CC=C6/C(C7=CC=C(OCC(C=C8)=CC=C8NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC(CCCCCN9C(C=CC9=O)=O)=O)=O)=O)C=C7)=C(C%10=CC=CC=C%10)/CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (59.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (1.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Syntheses of a PAC:
A. Chemical Synthesis of a PROTAC:
i. Attachment of a Linker (L2) to an E3 Ligase Binding Group (E3LB).
ii. Attachment of a protein binding moiety (PB) to an E3LB via a Linker (L2).
B. Preparation of L1-PROTAC:
iii. Attachment of Linker L1 to PROTAC.
C. Preparation of PAC:
iv. Attachment of Antibody (Ab) to PROTAC via Linker L1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.5970 mL | 2.9852 mL | 5.9704 mL | 14.9260 mL |
| 5 mM | 0.1194 mL | 0.5970 mL | 1.1941 mL | 2.9852 mL | |
| 10 mM | 0.0597 mL | 0.2985 mL | 0.5970 mL | 1.4926 mL | |
| 15 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL | 0.9951 mL | |
| 20 mM | 0.0299 mL | 0.1493 mL | 0.2985 mL | 0.7463 mL | |
| 25 mM | 0.0239 mL | 0.1194 mL | 0.2388 mL | 0.5970 mL | |
| 30 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4975 mL | |
| 40 mM | 0.0149 mL | 0.0746 mL | 0.1493 mL | 0.3731 mL | |
| 50 mM | 0.0119 mL | 0.0597 mL | 0.1194 mL | 0.2985 mL |
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