THZ2
Based on 6 publication(s) in Google Scholar
THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.03%
- CAS. Nr.: 1604810-84-5
- Formel: C31H28ClN7O2
- Molecular Weight:566.05
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) THZ2
More
Biologische Aktivität
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CDK7 13.9 nM (IC50) |
CDK1 96.9 nM (IC50) |
CDK2 222 nM (IC50) |
CDK5 134 nM (IC50) |
CDK9 194 nM (IC50) |
CDK8 6830 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
0.19 μM
Compound: 24; THZ2
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Cytotoxicity against human AGS cells assessed as reduction in cell viability
Cytotoxicity against human AGS cells assessed as reduction in cell viability
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[PMID: 31514062] |
| MGC-803 | IC50 |
0.74 μM
Compound: 24; THZ2
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Cytotoxicity against human MGC803 cells assessed as reduction in cell viability
Cytotoxicity against human MGC803 cells assessed as reduction in cell viability
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[PMID: 31514062] |
THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells. THZ2 at low nanomolar doses also efficiently suppresses the clonogenic growth of TNBC cells with IC50 of appr 10 nM. THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1604810-84-5
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Appearance Solid
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Molecular Weight 566.05
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Formel C31H28ClN7O2
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Color Light yellow to khaki
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SMILES
O=C(NC1=CC=CC(NC2=NC=C(Cl)C(C3=CNC4=C3C=CC=C4)=N2)=C1)C5=CC=CC(NC(/C=C/CN(C)C)=O)=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
Robust gene expression programs underlie recurrent cell states and phenotype switching in melanoma. [Abstract]2020 Aug;22(8):986-998. PMID: 32753671 -
Mol Cell
2025 Oct 17:S1097-2765(25)00785-3. PMID: 41109217 -
Biochim Biophys Acta Mol Basis Dis
Single-cell RNA sequencing and machine learning provide candidate drugs against drug-tolerant persister cells in colorectal cancer. [Abstract]2025 Mar;1871(3):167693. PMID: 39870146 -
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Lösungsmittel & Löslichkeit
DMSO : 21.67 mg/mL (38.28 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.17 mg/mL (3.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
Protokoll
For 96-well plate assay, cells are plated at the density of 2000 cells per well, and on the next day treated with THZ1 or THZ2 of various concentrations. After 48-hour incubation, cells are fixed and stained with crystal violet. The staining is then extracted by adding each well with 10% acetic acid, with absorbance measured at 590 nm with 750 nm as a reference.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Nude mice (CrTac:NCr-Foxn1nu) are γ-irradiated with a single dose of 400 rads six hours before transplantation of cells. Breast cancer cells are harvested and resupended in 40% Matrigel-Basement Membrane Matrix, LDEV-free, and then injected (100 μL per site) into the fourth pair of mammary fat pads of mice. Tumors are measured in two dimensions by using manual calipers. Tumor volume is calculated using the formula: V=0.5× length × width × width. Animal with tumor established (mean tumor volume of appr 200 mm3) are randomLy divided into two groups, which are then treated with vehicle (10% DMSO in D5W, 5% dextrose in water) or THZ2 (3 mg/mL, prepared in vehicle solutions) at the dose of 10 mg/kg intraperitoneally twice daily. Tumor volume is measure every 2-3 days. Upon harvesting tumors, tumors are cut into half, with one half fixed in formalin overnight and then in 70% ethanol for histopathology analysis, and the other half snap frozen in liquid nitrogen for immunoblotting.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7666 mL | 8.8331 mL | 17.6663 mL | 44.1657 mL |
| 5 mM | 0.3533 mL | 1.7666 mL | 3.5333 mL | 8.8331 mL | |
| 10 mM | 0.1767 mL | 0.8833 mL | 1.7666 mL | 4.4166 mL | |
| 15 mM | 0.1178 mL | 0.5889 mL | 1.1778 mL | 2.9444 mL | |
| 20 mM | 0.0883 mL | 0.4417 mL | 0.8833 mL | 2.2083 mL | |
| 25 mM | 0.0707 mL | 0.3533 mL | 0.7067 mL | 1.7666 mL | |
| 30 mM | 0.0589 mL | 0.2944 mL | 0.5889 mL | 1.4722 mL |
THZ2 Related Classifications
HY-12280 Related Classifications
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