HL-8
Based on 1 Customer Validation
HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)).
(Pink: PI3Kα ligand (HY-143277); Blue: VHL ligand (HY-138678); Black: linker (HY-W002042)).
For research use only. We do not sell to patients.
- Purity: 99.17%
- CAS No.: 2766352-64-9
- Formula: C57H59F2N11O9S2
- Molecular Weight:1144.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
HL-8 (1 nM) inhibits PI3Kα kinase by 49.75%[1].
HL-8 (10 μM; 72 h) inhibits the proliferation of HT-29, HCT-116, and Hela cells by 72.18%, 50.30%, and 96.33%, respectively[1].
HL-8 (10 μM; 2-24 h) significantly degrades PI3Kα and reduces phosphorylated AKT levels in Hela cells[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. 2766352-64-9
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Appearance Solid
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Molecular Weight 1144.27
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Formula C57H59F2N11O9S2
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Color White to off-white
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SMILES
COC1=NC=C(C=C1NS(=O)(C2=C(C=C(C=C2)F)F)=O)C3=CN4C(C5=NN=C(O5)C6=C(C=CC=C6)C(NCCCCCCC(N[C@@H](C(C)(C)C)C(N7C[C@H](C[C@@H]7C(NCC8=CC=C(C=C8)C9=C(N=CS9)C)=O)O)=O)=O)=O)=CN=C4C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (87.39 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 (2.18 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.
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.
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
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 0.8739 mL | 4.3696 mL | 8.7392 mL | 21.8480 mL |
| 5 mM | 0.1748 mL | 0.8739 mL | 1.7478 mL | 4.3696 mL | |
| 10 mM | 0.0874 mL | 0.4370 mL | 0.8739 mL | 2.1848 mL | |
| 15 mM | 0.0583 mL | 0.2913 mL | 0.5826 mL | 1.4565 mL | |
| 20 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0924 mL | |
| 25 mM | 0.0350 mL | 0.1748 mL | 0.3496 mL | 0.8739 mL | |
| 30 mM | 0.0291 mL | 0.1457 mL | 0.2913 mL | 0.7283 mL | |
| 40 mM | 0.0218 mL | 0.1092 mL | 0.2185 mL | 0.5462 mL | |
| 50 mM | 0.0175 mL | 0.0874 mL | 0.1748 mL | 0.4370 mL | |
| 60 mM | 0.0146 mL | 0.0728 mL | 0.1457 mL | 0.3641 mL | |
| 80 mM | 0.0109 mL | 0.0546 mL | 0.1092 mL | 0.2731 mL |
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