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| 10mg |
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| 25mg |
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Purity: ≥98%
THZ1-R is a novel and non-cysteine reactive analog of THZ1 which shows lower activity for CDK7 inhibition with a Kd of 142 nM for binding to CDK7. THZ1 is a novel, potent, selective and covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. THZ1 covalently modifies CDK7 by targeting C312 residue outside of the kinase domain, providing an unanticipated means of achieving covalent selectivity. THZ1 potently inhibits proliferation of Jurkat and Loucy T-ALL cell lines with IC50 values of 50nM and 0.55nM, respectively. In the kinase binding assay, THZ1 shows a good binding affinity with IC50 value of 3.2nM.
| ln Vitro |
THZ1-R, whose IC50 is 146 nM, exhibits a lower affinity for CDK7 than THZ1.
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| ln Vivo |
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| Animal Protocol |
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| References |
[1]. Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20
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| Molecular Formula |
C₃₁H₃₀CLN₇O₂
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| Molecular Weight |
568.07
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| CAS # |
1621523-07-6
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| Related CAS # |
THZ1;1604810-83-4;THZ1 Hydrochloride
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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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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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7603 mL | 8.8017 mL | 17.6035 mL | |
| 5 mM | 0.3521 mL | 1.7603 mL | 3.5207 mL | |
| 10 mM | 0.1760 mL | 0.8802 mL | 1.7603 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 .THZ1 demonstrates time-dependent inhibition of CDK7in vitroand covalent binding of intracellular CDK7.Nature.2014 Jul 31;511(7511):616-20. |
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 THZ1 covalently binds CDK7 C312.Nature.2014 Jul 31;511(7511):616-20. |
 THZ1 inhibits CDK12 but at higher concentrations compared to CDK7.Nature.2014 Jul 31;511(7511):616-20. |
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