(S,R,S)-AHPC-C6-PEG3-C4-Cl
Based on 1 publication(s) in Google Scholar
(S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
For research use only. We do not sell to patients.
- Purity: 97.01%
- CAS No.: 1835705-55-9
- Formula: C38H59ClN4O7S
- Molecular Weight:751.42
-
Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) (S,R,S)-AHPC-C6-PEG3-C4-Cl
MoreAll E3 Ligase Ligand-Linker Conjugates Isoforms
More
Biological Activity
|
VHL |
(S,R,S)-AHPC-C6-PEG3-C4-Cl uses the cereblon ligand[1]. The linker is 6-2-2-6. The linkers contain a mixture of hydrophobic and hydrophilic moieties to balance the hydrophobicity/hydrophilicity of the resulting hybrid compounds. PROTACs that induce the degradation of an oncogenic tyrosine kinase, BCR-ABL has been developed. (S,R,S)-AHPC-C6-PEG3-C4-Cl can be attached to potent TKIs (bosutinib and dasatinib) that mediate the degradation of c-ABL and BCR-ABL by hijacking either CRBN or VHL E3 ubiquitin ligase [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1835705-55-9
-
Appearance Oil
-
Molecular Weight 751.42
-
Formula C38H59ClN4O7S
-
Color Colorless to light yellow
-
SMILES
O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCCOCCOCCOCCCCCCCl)=O)=O)C[C@H](O)C1)NCC2=CC=C(C3=C(C)N=CS3)C=C2
-
Synonyms
VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Solvent & Solubility
DMSO : 100 mg/mL (133.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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.
Purity & Documentation
-
Data Sheet (270 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
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. 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 | 1.3308 mL | 6.6541 mL | 13.3081 mL | 33.2703 mL |
| 5 mM | 0.2662 mL | 1.3308 mL | 2.6616 mL | 6.6541 mL | |
| 10 mM | 0.1331 mL | 0.6654 mL | 1.3308 mL | 3.3270 mL | |
| 15 mM | 0.0887 mL | 0.4436 mL | 0.8872 mL | 2.2180 mL | |
| 20 mM | 0.0665 mL | 0.3327 mL | 0.6654 mL | 1.6635 mL | |
| 25 mM | 0.0532 mL | 0.2662 mL | 0.5323 mL | 1.3308 mL | |
| 30 mM | 0.0444 mL | 0.2218 mL | 0.4436 mL | 1.1090 mL | |
| 40 mM | 0.0333 mL | 0.1664 mL | 0.3327 mL | 0.8318 mL | |
| 50 mM | 0.0266 mL | 0.1331 mL | 0.2662 mL | 0.6654 mL | |
| 60 mM | 0.0222 mL | 0.1109 mL | 0.2218 mL | 0.5545 mL | |
| 80 mM | 0.0166 mL | 0.0832 mL | 0.1664 mL | 0.4159 mL | |
| 100 mM | 0.0133 mL | 0.0665 mL | 0.1331 mL | 0.3327 mL |
(S,R,S)-AHPC-C6-PEG3-C4-Cl Related Classifications
HY-103605 Related Classifications
Powered by Bioz