Q901 TFA
Based on 1 Customer Validation
Q901 TFA (CDK7-IN-21 TFA) is a selective covalent ATP-competitive CDK7 inhibitor with an IC50 value of 10 nM against human CDK7. Q901 TFA inhibits MYC/E2F-dependent oncogenic transcription, the RNAPII transition from initiation to elongation, and DNA damage repair, stabilizes TOP1-DNA protein crosslinks, and induces DNA damage. Q901 TFA sensitizes tumors to topoisomerase I inhibitors and TOP1 inhibitor-based antibody-drug conjugates. Q901 TFA shows additive or synergistic tumor growth inhibition in solid tumor models in combination with PARP inhibitors, SERDs, ER PROTAC degraders, or anti-PD-1 antibodies. Q901 TFA can be used for research on cancers such as ovarian cancer and lung cancer.
For research use only. We do not sell to patients.
- Purity : 98.55%
- Formula: C35H37F4N9O4
- Molecular Weight:723.72
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Storage:
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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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CDK7 10 nM (IC50) |
Top1 |
In Vitro
Q901 (72-120 h) TFA potently inhibits MCF-7 proliferation, with IC50 values of 95, 16, and 5 nM at 72, 96, and 120 h, respectively[3].
Q901 (100 nM; 1-24 h) TFA reduces promoter-proximal RNAPII and traps CDK7 at promoters in MCF-7 cells[3].
Q901 (100 nM; 1-24 h) TFA decreases promoter occupancy of MYC and E2F1 and reduces E2F1 expression in MCF-7 cells[3].
Q901 (100 nM; 4-24 h) TFA impairs enhancer activity in MCF-7 cells but has no strong preferential effect on super-enhancer targets[3].
Q901 (10-1000 nM; 24-72 h) TFA induces DNA damage and increases γH2AX expression in MCF-7 cells[3].
Q901 (100 nM; 30 min-24 h) TFA stabilizes TOP1-DPC and inhibits DDR gene expression in MCF-7 cells[3].
Q901 (72 h) TFA enhances the antiproliferative activity of Topotecan (TPT) (HY-13768) in H82, DMS53, and H446 SCLC cells[3].
Q901 (72 h) TFA sensitizes HCT116 cells to T-DXd (HY-138298A) in vitro, with an IC50 of 8.4 nM for Q901[3].
Q901 (72 h) TFA enhances the antiproliferative activity of Sacituzumab govitecan (SG) (HY-132254) in H292 cells, with an IC50 of 12 nM for Q901[3].
Q901 (100 μM; 72 h) TFA inhibits the viability of H82, A2780, and MCF7 cells within 72 h in a dilution series starting at 100 μM[4].
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:Increased γH2AX levels over time in a dose-dependent manner.
Pronounced P-H2AX induction was observed at 48 h with 1000 nM and at 72 h with 1000 nM.
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Cell Line:A2780 cells
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Concentration:6 nM
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Incubation Time:4 h (exposure); washout at 0, 4, 24, and 48 h
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Result:Free CDK7 levels were analyzed by immunoblotting at 0, 4, 24, and 48 h after washout.
CDK7 engagement was observed.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude[3]
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Dosage:10 mg/kg
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Administration:i.p.; once daily
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Result:On day 28, 81% tumor growth inhibition was achieved; 102% tumor growth inhibition was achieved in the T-DXd-containing arm.
Tumors resumed growth by ∼11 days after dosing ended, whereas the T-DXd-containing arm maintained tumor suppression throughout the study.
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Animal Model:BALB/c nude[3]
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Dosage:10 mg/kg
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Administration:i.p.; once daily
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Result:By day 28, 80% tumor growth inhibition was achieved; 90% tumor growth inhibition was achieved in the SG-containing arm.
Sustained tumor growth inhibition was maintained throughout the study period, with slightly higher efficacy in the SG-containing arm.
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Animal Model:BALB/c nude[3]
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Dosage:3 mg/kg
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Administration:i.p.; once daily
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Result:By day 28, 61% tumor growth inhibition was achieved; 92% tumor growth inhibition was achieved in the SG-containing arm.
Sustained tumor growth inhibition was maintained throughout the study period.
Chemical Information
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Appearance Solid
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Molecular Weight 723.72
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
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.
Purity & Documentation
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Data Sheet (283 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 |
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| 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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