Q901 TFA
Based on 1 Customer Validation
Q901 (CDK7-IN-21) TFA is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 TFA disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 TFA can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 TFA can be used for the research of cancer, such as colon cancer and lung cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 98.55%
- 화학식: C35H37F4N9O4
- 분자량:723.72
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보관:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
CDK7 10 nM (IC50) |
In Vitro
Q901 (72-120 h) TFA 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) TFA 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) TFA 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) TFA 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 TFA 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. Further protocols information, click here.
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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.
In Vivo
Q901 (3-10 mg/kg, i.p., once daily) TFA 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.
Chemical Information
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Appearance Solid
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분자량 723.72
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화학식 C35H37F4N9O4
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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.OC(C(F)(F)F)=O
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Synonyms
CDK7-IN-21 TFA
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
용액&용해도
In Vitro:
DMSO : 50 mg/mL (69.09 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 (stored under nitrogen, away from moisture). 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 (stored under nitrogen, away from moisture). 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)
In Vivo:
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 (3.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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 (3.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (stored under nitrogen, away from moisture). 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 | 1.3817 mL | 6.9087 mL | 13.8175 mL | 34.5437 mL |
| 5 mM | 0.2763 mL | 1.3817 mL | 2.7635 mL | 6.9087 mL | |
| 10 mM | 0.1382 mL | 0.6909 mL | 1.3817 mL | 3.4544 mL | |
| 15 mM | 0.0921 mL | 0.4606 mL | 0.9212 mL | 2.3029 mL | |
| 20 mM | 0.0691 mL | 0.3454 mL | 0.6909 mL | 1.7272 mL | |
| 25 mM | 0.0553 mL | 0.2763 mL | 0.5527 mL | 1.3817 mL | |
| 30 mM | 0.0461 mL | 0.2303 mL | 0.4606 mL | 1.1515 mL | |
| 40 mM | 0.0345 mL | 0.1727 mL | 0.3454 mL | 0.8636 mL | |
| 50 mM | 0.0276 mL | 0.1382 mL | 0.2763 mL | 0.6909 mL | |
| 60 mM | 0.0230 mL | 0.1151 mL | 0.2303 mL | 0.5757 mL |
Q901 TFA Related Classifications
HY-153278A Related Classifications
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