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THZ1-R

カタログ番号GC37786

THZ1-R は THZ1 の非システイン反応性類似体であり、CDK7 阻害活性の低下を示します。 THZ1-R は 142 nM の Kd で CDK7 に結合します。

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THZ1-R 化学構造

Cas No.: 1621523-07-6

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$406.00
在庫あり
1mg
$139.00
在庫あり
5mg
$324.00
在庫あり
10mg
$510.00
在庫あり
50mg
$1,530.00
在庫あり
100mg
$2,132.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of THZ1-R

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. CDK7|146 nM (IC50)

THZ1-R shows lower affinity at CDK7 than THZ1, with IC50 of 146 nM[1].

[1]. Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.

Chemical Properties of THZ1-R

Cas No. 1621523-07-6 SDF
Canonical 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
Formula C31H30ClN7O2 M.Wt 568.07
溶解度 DMSO: ≥ 100 mg/mL (176.03 mM); Water: < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of THZ1-R

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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 0.176 mL 0.8802 mL 1.7603 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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