2. Cell Cycle/DNA Damage Apoptosis
  3. CDK DNA/RNA Synthesis c-Myc Early 2 Factor (E2F) Topoisomerase
  4. 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.

For research use only. We do not sell to patients.

Q901

Q901 Chemical Structure

CAS No. : 2766124-39-2

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Q901 Related Antibodies

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Topoisomerase Topo I Topo II DNA gyrase

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  • Purity & Documentation

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Description

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[1].

IC50 & Target[1]

CDK7

10 nM (IC50)

In Vitro

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.

Q901 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10, 100, 1000 nM
Incubation Time: 24, 48, 72 h
Result: Does-and time-dependently increased p-H2AX levels at 24 and 48 h.
Increased p-H2AX levels at 72 h.
In Vivo

Q901 (10 mg/kg, i.p., once daily, 30 days) inhibits tumor growth in HCT116 colon cancer xenograft mice, and significantly enhances tumor growth inhibition combined with T-DXd (10 mg/kg, i.v., single injection on day 0) (TGI = 102%), achieving sustained tumor suppression[1].
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.

Animal Model: HCT116 colon cancer xenograft mice models[1]
Dosage: 10 mg/kg
Administration: Intraperitoneally injection, once daily, 30 days
Result: Reduced tumor volume alone and significantly reduced volume to near 0 combined with T-DXd.
Molecular Weight

609.70

Formula

C33H36FN9O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6402 mL 8.2008 mL 16.4015 mL
5 mM 0.3280 mL 1.6402 mL 3.2803 mL
View the 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.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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Volume (final)

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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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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 1.6402 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
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Q901 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Q9012766124-39-2CDK7-IN-21Q 901Q-901CDKDNA/RNA Synthesisc-MycEarly 2 Factor (E2F)TopoisomeraseCyclin dependent kinaseMycCDK5CDK2proteasome complexpoly-ubiquitinationCDK7CDK1cancer cellsA2780 human ovarian cancer cellsInhibitorinhibitorinhibit

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