Hsp90-Cdc37-IN-3
Based on 1 Customer Validation
Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis.
For research use only. We do not sell to patients.
- Purity: 98.09%
- CAS No.: 2361009-68-7
- Formula: C35H44ClN3O6
- Molecular Weight:638.19
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Hsp90-Cdc37 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>100 μM
Compound: 9
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Antiproliferative activity against human A549 cells expressing Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 35238566] |
| A549 | IC50 |
>100 μM
Compound: 9
|
Antiproliferative activity against human A549 cells expressing Hsp90 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing Hsp90 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 35238566] |
| A549 | IC50 |
>100 μM
Compound: 9
|
Antiproliferative activity against human A549 cells expressing Hsp90-Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing Hsp90-Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 35238566] |
| A549 | IC50 |
0.54 μM
Compound: 9
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 35238566] |
| HCT-116 | IC50 |
0.59 μM
Compound: 9
|
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 35238566] |
| MDA-MB-231 | IC50 |
0.57 μM
Compound: 9
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 35238566] |
| U2OS | IC50 |
0.57 μM
Compound: 9
|
Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 35238566] |
Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50 values of 0.54, 0.59, 0.57, and 0.57 µM against A549, HTC116, U2OS, and MDA-MB231 cells, respectively[1].
Hsp90-Cdc37-IN-3 (0-5 µM, 12 h) inhibits Hsp90−Cdc37 and influences the function of apoptosis-related proteins by covalently combining with both Hsp90 and Cdc37[1].
Hsp90-Cdc37-IN-3 (0-0.8 µM, 48 h) induces apoptosis significantly in A549 cells[1].
Hsp90-Cdc37-IN-3 (0-0.4 µM, 24 h) arrests the cell cycle in the G0/G1 phase in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549
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Concentration:1.25, 2.5, and 5 µM
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Incubation Time:12 h
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Result:Downregulated the levels of Hsp90−Cdc37 clients (p-Akt and Cdk4) in a dose-dependent manner, and the levels of apoptosis-related proteins (Bax, Bcl-2, cleaved caspase-3, and cleaved PARP) were significantly regulated.
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Cell Line:A549
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Concentration:0.2, 0.4, and 0.8 μM
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Incubation Time:48 h
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Result:Induced apoptosis significantly.
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Cell Line:A549
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Concentration:0.1, 0.2, and 0.4 μM
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Incubation Time:24 h
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Result:Arrested the cell cycle in the G0/G1 phase in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice at 6 weeks old[1].
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Dosage:0.5 mg/kg or 1 mg/kg. Mice were inoculated subcutaneously with A549 cells (1*107 in 100 μL of PBS for each mouse).
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Administration:Intraperitoneal injection, once a day, 21 days
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Result:Decreased tumor weight and enhanced TIR without show toxicity.
Chemical Information
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CAS No. 2361009-68-7
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Appearance Solid
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Molecular Weight 638.19
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Formula C35H44ClN3O6
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Color Light yellow to yellow
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SMILES
O=C1C(O)=C(C2=CC=C3[C@](C)([C@]4(CC[C@]3(C2=C1)C)C)CC[C@@]5([C@@]4([H])C[C@](C(OCCCN6C(Cl)=NC([N+]([O-])=O)=C6)=O)(CC5)C)C)C
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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 (156.69 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 (3.92 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (276 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 | 1.5669 mL | 7.8347 mL | 15.6693 mL | 39.1733 mL |
| 5 mM | 0.3134 mL | 1.5669 mL | 3.1339 mL | 7.8347 mL | |
| 10 mM | 0.1567 mL | 0.7835 mL | 1.5669 mL | 3.9173 mL | |
| 15 mM | 0.1045 mL | 0.5223 mL | 1.0446 mL | 2.6116 mL | |
| 20 mM | 0.0783 mL | 0.3917 mL | 0.7835 mL | 1.9587 mL | |
| 25 mM | 0.0627 mL | 0.3134 mL | 0.6268 mL | 1.5669 mL | |
| 30 mM | 0.0522 mL | 0.2612 mL | 0.5223 mL | 1.3058 mL | |
| 40 mM | 0.0392 mL | 0.1959 mL | 0.3917 mL | 0.9793 mL | |
| 50 mM | 0.0313 mL | 0.1567 mL | 0.3134 mL | 0.7835 mL | |
| 60 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6529 mL | |
| 80 mM | 0.0196 mL | 0.0979 mL | 0.1959 mL | 0.4897 mL | |
| 100 mM | 0.0157 mL | 0.0783 mL | 0.1567 mL | 0.3917 mL |