YK-2168
Based on 1 Customer Validation
YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. YK-2168 inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses expression of CDK9-regulated genes including MYC and Mcl1, and inhibits tumor growth in CDX mice models. YK-2168 can be used for the research of cancer, such as leukemia.
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- Purity: 98.05%
- CAS No.: 2571068-74-9
- 화학식: C16H18ClN5
- 분자량:315.80
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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CDK9 5.9 nM (IC50) |
CDK2 266.9 nM (IC50) |
CDK1 427.7 nM (IC50) |
YK-2168 potently inhibits purified CDK9 enzymatic activity with an IC50 of 5.9 nM, and exhibits 72.5-fold and 45.2-fold selectivity over purified CDK1 (IC50 = 427.7 nM) and CDK2 (IC50 = 266.9 nM), respectively[1].
YK-2168 inhibits proliferation of MV4-11 leukemia cells with an IC50 of 53.4 nM[1].
YK-2168 30 μM) does not inhibit hERG channel activity at concentrations up to 30 μM[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.
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Animal Model:CD-1 mouse cell-derived xenograft
(CDX) model of leukemia (MV4-11) cell line[1] -
Dosage:5, 10,15 mg/kg
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Administration:i.v.; once weekly; 4 weeks
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Result:Achieved a tumor growth inhibition (TGI) of 80% at 10 mg/kg.
Induced dose-dependent reduction of pS2-RNA Pol II CTD levels in tumor tissue.
Suppressed CDK9-regulated MYC and Mcl1 protein expression lasting up to 24 hours post-treatment.
Upregulated cleaved caspase 3 in a time-dependent manner, indicating induced apoptosis.
Showed body weight changes statistically indistinguishable from vehicle controls, indicating good safety.
Chemical Information
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CAS No. 2571068-74-9
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Appearance Solid
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분자량 315.80
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화학식 C16H18ClN5
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Color Off-white to light yellow
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SMILES
ClC1=CN=C(NC(C2CCNCC2)=C3)C3=C1C4=CN(C)N=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (316.66 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 5 mg/mL (15.83 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
순도&문서
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Data Sheet (275 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL | 79.1640 mL |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL | 15.8328 mL | |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 mL | 7.9164 mL | |
| 15 mM | 0.2111 mL | 1.0555 mL | 2.1110 mL | 5.2776 mL | |
| 20 mM | 0.1583 mL | 0.7916 mL | 1.5833 mL | 3.9582 mL | |
| 25 mM | 0.1267 mL | 0.6333 mL | 1.2666 mL | 3.1666 mL | |
| 30 mM | 0.1056 mL | 0.5278 mL | 1.0555 mL | 2.6388 mL | |
| 40 mM | 0.0792 mL | 0.3958 mL | 0.7916 mL | 1.9791 mL | |
| 50 mM | 0.0633 mL | 0.3167 mL | 0.6333 mL | 1.5833 mL | |
| 60 mM | 0.0528 mL | 0.2639 mL | 0.5278 mL | 1.3194 mL | |
| 80 mM | 0.0396 mL | 0.1979 mL | 0.3958 mL | 0.9896 mL | |
| 100 mM | 0.0317 mL | 0.1583 mL | 0.3167 mL | 0.7916 mL |
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