CH5015765
Based on 1 Customer Validation
CH5015765 is an orally available Hsp90 inhibitor bound to the N-terminal ATP binding site, with a dissociation constant of 3.4 nM, CH5015765 exerts antiproliferative activity against human cancer cell lines, with IC50 values of 0.46 μM for HCT116 colorectal cancer cells and 0.57 μM for NCI-N87 gastric cancer cells. CH5015765 can be used for the study of cancer.
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- Pureté : 98.01%
- CAS No.: 959766-47-3
- Formule: C16H13ClN4OS
- Masse moléculaire:344.82
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Stockage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
HSP90 3.4 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.46 μM
Compound: CH-5015765
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Growth inhibition of human HCT116 cells
Growth inhibition of human HCT116 cells
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[PMID: 21875802] |
| NCI-N87 | IC50 |
0.57 μM
Compound: 12
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Antiproliferative activity against human NCI-N87 cells after 4 days by CCK-8 assay
Antiproliferative activity against human NCI-N87 cells after 4 days by CCK-8 assay
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[PMID: 35033884] |
In Vitro
CH5015765 (4 days) exerts in vitro antiproliferative activity against human cancer cell lines, with IC50 values of 0.46 μM for HCT116 colorectal cancer cells and 0.57 μM for NCI-N87 gastric cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human NCI-N87 gastric cancer cells were subcutaneously implanted into the right flanks of athymic nude (BALB/c nu/nu) mice [1]
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Dosage:400 mg/kg
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Administration:p.o., once daily for 11 consecutive days, Days 11-21
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Result:Exerted moderate antitumor efficacy in SCID mice bearing human NCI-N87 gastric cancer xenografts, with a tumor growth inhibition (TGI) rate of 54%.
Chemical Information
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CAS No. 959766-47-3
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Appearance Solid
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Masse moléculaire 344.82
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Formule C16H13ClN4OS
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Color Light yellow to yellow
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SMILES
NC1=NC(C2=C(Cl)C=C3C4=C2C=CC=C4COC3)=NC(SC)=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (145.00 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 (protect from light, 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 (protect from light, 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)
In Vivo:
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 (7.25 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 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.
In Vivo Dissolution Calculator
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 (protect from light, 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.
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
[1]. Suda A, et al. Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors. Bioorg Med Chem. 2014 Jan 15;22(2):892-905. [Content Brief]
[2]. Atsushi Suda, et al. Design and synthesis of novel macrocyclic 2-amino-6-arylpyrimidine Hsp90 inhibitors. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1136-41. [Content Brief]
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 (protect from light, 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 | 2.9001 mL | 14.5003 mL | 29.0006 mL | 72.5016 mL |
| 5 mM | 0.5800 mL | 2.9001 mL | 5.8001 mL | 14.5003 mL | |
| 10 mM | 0.2900 mL | 1.4500 mL | 2.9001 mL | 7.2502 mL | |
| 15 mM | 0.1933 mL | 0.9667 mL | 1.9334 mL | 4.8334 mL | |
| 20 mM | 0.1450 mL | 0.7250 mL | 1.4500 mL | 3.6251 mL | |
| 25 mM | 0.1160 mL | 0.5800 mL | 1.1600 mL | 2.9001 mL | |
| 30 mM | 0.0967 mL | 0.4833 mL | 0.9667 mL | 2.4167 mL | |
| 40 mM | 0.0725 mL | 0.3625 mL | 0.7250 mL | 1.8125 mL | |
| 50 mM | 0.0580 mL | 0.2900 mL | 0.5800 mL | 1.4500 mL | |
| 60 mM | 0.0483 mL | 0.2417 mL | 0.4833 mL | 1.2084 mL | |
| 80 mM | 0.0363 mL | 0.1813 mL | 0.3625 mL | 0.9063 mL | |
| 100 mM | 0.0290 mL | 0.1450 mL | 0.2900 mL | 0.7250 mL |
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