THZ1-R
Based on 3 publication(s) in Google Scholar
THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.
For research use only. We do not sell to patients.
- Purity: 98.05%
- CAS No.: 1621523-07-6
- Formula: C31H30ClN7O2
- Molecular Weight:568.07
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Publications Citing Use of MedChemExpress (MCE) THZ1-R
More
Biological Activity
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CDK7 146 nM (IC50) |
Chemical Information
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CAS No. 1621523-07-6
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Appearance Solid
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Molecular Weight 568.07
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Formula C31H30ClN7O2
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Color Light yellow to yellow
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SMILES
ClC1=CN=C(NC2=CC(NC(C3=CC=C(NC(CCCN(C)C)=O)C=C3)=O)=CC=C2)N=C1C4=CNC5=CC=CC=C54
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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 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cancer Discov
CDK7 Inhibition Suppresses Castration-Resistant Prostate Cancer through MED1 Inactivation. [Abstract]2019 Nov;9(11):1538-1555. PMID: 31466944 -
Cell Death Dis
CDK7 inhibitor THZ1 inhibits MCL1 synthesis and drives cholangiocarcinoma apoptosis in combination with BCL2/BCL-XL inhibitor ABT-263. [Abstract]2019 Aug 9;10(8):602. PMID: 31399555 -
Proc Natl Acad Sci U S A
CDK7 inhibition suppresses aberrant hedgehog pathway and overcomes resistance to smoothened antagonists. [Abstract]2019 Jun 25;116(26):12986-12995. PMID: 31182587
Solvent & Solubility
DMSO : ≥ 100 mg/mL (176.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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 (4.40 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.
Protocol
Cells are seeded in 384-well microplates at 15% confluency in medium with 5% FBS and penicillin/streptavidin. Cells are treated with THZ1 or DMSO for 72 hrs and cell viability is determined using resazurin.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 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, 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 |
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| DMSO | 1 mM | 1.7603 mL | 8.8017 mL | 17.6035 mL | 44.0087 mL |
| 5 mM | 0.3521 mL | 1.7603 mL | 3.5207 mL | 8.8017 mL | |
| 10 mM | 0.1760 mL | 0.8802 mL | 1.7603 mL | 4.4009 mL | |
| 15 mM | 0.1174 mL | 0.5868 mL | 1.1736 mL | 2.9339 mL | |
| 20 mM | 0.0880 mL | 0.4401 mL | 0.8802 mL | 2.2004 mL | |
| 25 mM | 0.0704 mL | 0.3521 mL | 0.7041 mL | 1.7603 mL | |
| 30 mM | 0.0587 mL | 0.2934 mL | 0.5868 mL | 1.4670 mL | |
| 40 mM | 0.0440 mL | 0.2200 mL | 0.4401 mL | 1.1002 mL | |
| 50 mM | 0.0352 mL | 0.1760 mL | 0.3521 mL | 0.8802 mL | |
| 60 mM | 0.0293 mL | 0.1467 mL | 0.2934 mL | 0.7335 mL | |
| 80 mM | 0.0220 mL | 0.1100 mL | 0.2200 mL | 0.5501 mL | |
| 100 mM | 0.0176 mL | 0.0880 mL | 0.1760 mL | 0.4401 mL |
THZ1-R Related Classifications
HY-19988 Related Classifications
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