CDK9-IN-7
Based on 1 Customer Validation
CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
For research use only. We do not sell to patients.
- Purity: 98.05%
- CAS No.: 2369981-71-3
- Formula: C29H37N7O2S
- Molecular Weight:547.71
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
CDK9/cyclinT1 11 nM (IC50) |
CDK4/cyclin D 148 nM (IC50) |
CDK6/cyclinD 145 nM (IC50) |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.45 μM
Compound: 21e
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| CCRF-CEM | IC50 |
>10 μM
Compound: 21e
|
Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| HCC827 | IC50 |
1.071 μM
Compound: 21e
|
Antiproliferative activity against human HCC827 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human HCC827 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| HeLa | IC50 |
1.85 μM
Compound: 21e
|
Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| Hep 3B2 | IC50 |
5.61 μM
Compound: 21e
|
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| HepG2 | IC50 |
3.861 μM
Compound: 21e
|
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| Jurkat | IC50 |
3.427 μM
Compound: 21e
|
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| MCF7 | IC50 |
1.739 μM
Compound: 21e
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| MDA-MB-231 | IC50 |
3.045 μM
Compound: 21e
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| NCI-H1299 | IC50 |
0.203 μM
Compound: 21e
|
Antiproliferative activity against human H1299 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human H1299 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| NCI-H1975 | IC50 |
0.837 μM
Compound: 21e
|
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| PC-9 | IC50 |
0.947 μM
Compound: 21e
|
Antiproliferative activity against human PC9 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human PC9 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| SiHa | IC50 |
1.809 μM
Compound: 21e
|
Antiproliferative activity against human SiHa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human SiHa cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
| U-937 | IC50 |
1.988 μM
Compound: 21e
|
Antiproliferative activity against human U937 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human U937 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay
|
[PMID: 31376566] |
CDK9-IN-7 displays exceptional potency against NSCLC cell lines, especial A549 and H1299 with IC50 values less than 0.5 µM. In the drug-resistant NSCLC cell line H1975, CDK9-IN-7 also exhibits good inhibition potency with an IC50 value of 0.837 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2369981-71-3
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Appearance Solid
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Molecular Weight 547.71
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Formula C29H37N7O2S
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Color Light yellow to yellow
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SMILES
O=C(N(C)C)C1=CC2=CN=C(NC3=CC=C(NC(CCCCCCCN=C=S)=O)C=C3)N=C2N1C4CCCC4
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 62.5 mg/mL (114.11 mM; Need ultrasonic; 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: ≥ 2.08 mg/mL (3.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation
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Data Sheet (270 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)
- 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 | 1.8258 mL | 9.1289 mL | 18.2578 mL | 45.6446 mL |
| 5 mM | 0.3652 mL | 1.8258 mL | 3.6516 mL | 9.1289 mL | |
| 10 mM | 0.1826 mL | 0.9129 mL | 1.8258 mL | 4.5645 mL | |
| 15 mM | 0.1217 mL | 0.6086 mL | 1.2172 mL | 3.0430 mL | |
| 20 mM | 0.0913 mL | 0.4564 mL | 0.9129 mL | 2.2822 mL | |
| 25 mM | 0.0730 mL | 0.3652 mL | 0.7303 mL | 1.8258 mL | |
| 30 mM | 0.0609 mL | 0.3043 mL | 0.6086 mL | 1.5215 mL | |
| 40 mM | 0.0456 mL | 0.2282 mL | 0.4564 mL | 1.1411 mL | |
| 50 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9129 mL | |
| 60 mM | 0.0304 mL | 0.1521 mL | 0.3043 mL | 0.7607 mL | |
| 80 mM | 0.0228 mL | 0.1141 mL | 0.2282 mL | 0.5706 mL | |
| 100 mM | 0.0183 mL | 0.0913 mL | 0.1826 mL | 0.4564 mL |