الصفحة الرئيسية>>YKL-5-124 TFA

YKL-5-124 TFA

رقم الكتالوجGC39462

YKL-5-124 TFA هو مثبط CDK7 قوي وانتقائي ولا رجوع فيه وتساهمي مع IC50s من 53.5 نانومتر و 9.7 نانومتر لـ CDK7 و CDK7 / Mat1 / CycH ، على التواليYKL-5-124 TFA هو أكثر من 100 ضعف انتقائي لـ CDK7 من CDK9 و CDK2 ، وغير نشط ضد CDK12 و CDK13يحث YKL-5-124 TFA على توقيف قوي لدورة الخلية ، ويمنع التعبير الجيني الذي يحركه E2F ، ويظهر تأثيرًا ضئيلًا على حالة فسفرة RNA polymerase II

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YKL-5-124 TFA التركيب الكيميائي

Cas No.: 2748220-93-9

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
317٫00
متوفر
1mg
162٫00
متوفر
5mg
229٫00
متوفر
10mg
391٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of YKL-5-124 TFA

YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selectivity for CDK7 than CDK9 and CDK2 and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, and inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1].

[1]. Olson CM, et al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10.

Chemical Properties of YKL-5-124 TFA

Cas No. 2748220-93-9 SDF
Canonical SMILES CC1(C)N(C(N[C@@H](C2=CC=CC=C2)CN(C)C)=O)CC3=C1NN=C3NC(C4=CC=C(NC(C=C)=O)C=C4)=O.FC(F)(C(O)=O)F
Formula C30H34F3N7O5 M.Wt 629.63
الذوبان DMSO: ≥ 100 mg/mL (158.82 mM) 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 YKL-5-124 TFA

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.5882 mL 7.9412 mL 15.8823 mL
5 mM 0.3176 mL 1.5882 mL 3.1765 mL
10 mM 0.1588 mL 0.7941 mL 1.5882 mL
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In vivo Formulation Calculator (Clear solution) of YKL-5-124 TFA

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 6 reference(s) in Google Scholar.)

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