Q901
Q901 (CDK7-IN-21) is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 can be used for the research of cancer, such as colon cancer and lung cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2766124-39-2
- 分子式: C33H36FN9O2
- 分子量:609.70
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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CDK7 10 nM (IC50) |
Q901 (72-120 h) inhibits the proliferation of MCF-7 breast cancer cells with IC50 values of 95 nM (72 h), 16 nM (96 h) and 5 nM (120 h)[1].
Q901 (100 nM, 1-24 h) traps CDK7 at promoter-proximal regions, reduces chromatin-bound RNAPII and its Ser5/Ser2 phosphorylation, and downregulates MYC/E2F-driven transcription programs[1].
Q901 (10-1000 nM, 24-72 h) downregulates DNA damage repair (DDR) genes and increases p-H2AX levels, inducing DNA damage accumulation in MCF-7 cells[1].
Q901 (1 μM, 24 h) reduces ubiquitination of TOP1-DPCs induced by TPT (1 μM, 0.5-2 h) and prolongs the stability of TOP1-DPCs in MCF-7 cells[1].
Q901 combined with Topotecan (HY-13768), T-DXd (HY-138298) and Sacituzumab govitecan (HY-132254) synergistically inhibits the proliferation of H82, DMS53 small cell lung cancer cells, HCT116 colon cancer cells and H292 lung cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:10, 100, 1000 nM
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Incubation Time:24, 48, 72 h
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Result:Does-and time-dependently increased p-H2AX levels at 24 and 48 h.
Increased p-H2AX levels at 72 h.
Q901 (3-10 mg/kg, i.p., once daily) inhibits tumor growth in H292 lung cancer xenograft mice and significantly enhances tumor growth inhibition combined with Sacituzumab govitecan (3-10 mg/kg, i.v., on day 1 and 8) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 colon cancer xenograft mice models[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneally injection, once daily, 30 days
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Result:Reduced tumor volume alone and significantly reduced volume to near 0 combined with T-DXd.
化学情報
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CAS 番号 2766124-39-2
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性状 Solid
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分子量 609.70
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分子式 C33H36FN9O2
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Color White to off-white
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SMILES
C=C(F)C(NC(C=C1)=CC2=C1C(C(C=CC=C3)=C3CNC(N4N=C5)=NC(NC[C@@H]6[C@H](CNCC6)O)=NC4=C5C(C)C)=NC=C2)=O
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別名
CDK7-IN-21
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (164.02 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: 2.5 mg/mL (4.10 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.10 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 1.6402 mL | 8.2008 mL | 16.4015 mL | 41.0038 mL |
| 5 mM | 0.3280 mL | 1.6402 mL | 3.2803 mL | 8.2008 mL | |
| 10 mM | 0.1640 mL | 0.8201 mL | 1.6402 mL | 4.1004 mL | |
| 15 mM | 0.1093 mL | 0.5467 mL | 1.0934 mL | 2.7336 mL | |
| 20 mM | 0.0820 mL | 0.4100 mL | 0.8201 mL | 2.0502 mL | |
| 25 mM | 0.0656 mL | 0.3280 mL | 0.6561 mL | 1.6402 mL | |
| 30 mM | 0.0547 mL | 0.2734 mL | 0.5467 mL | 1.3668 mL | |
| 40 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL | |
| 50 mM | 0.0328 mL | 0.1640 mL | 0.3280 mL | 0.8201 mL | |
| 60 mM | 0.0273 mL | 0.1367 mL | 0.2734 mL | 0.6834 mL | |
| 80 mM | 0.0205 mL | 0.1025 mL | 0.2050 mL | 0.5125 mL | |
| 100 mM | 0.0164 mL | 0.0820 mL | 0.1640 mL | 0.4100 mL |
Q901 関連分類
HY-153278 関連分類
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