2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK12-IN-E9

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.

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

CDK12-IN-E9 Chemical Structure

CDK12-IN-E9 Chemical Structure

CAS No. : 2020052-55-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 440 In-stock
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Solid
1 mg USD 160 In-stock
5 mg USD 400 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2700 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CDK12-IN-E9 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CDK12-IN-E9

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM[1].

IC50 & Target[1]

CDK12

 

CDK9/cyclinT1

23.9 nM (IC50)

cdk2/cyclin A

932 nM (IC50)

CDK7/Cyclin H/MNAT1

1210 nM (IC50)

In Vitro

CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM[1].
CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression[1].
CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CDK12-IN-E9 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells
Concentration: 10 nM-10 μM
Incubation Time: 72 hours
Result: Showed potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM.

Western Blot Analysis[1]

Cell Line: Kelly, PC-9, and NCI-H82 cells
Concentration: 0 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM
Incubation Time: 6 hours
Result: Led to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models.
Molecular Weight

434.53

Formula

C24H30N6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(NC1=CC=CC(NC2=CC(N3[C@H](CCO)CCCC3)=NC4=C(CC)C=NN24)=C1)=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 : 125 mg/mL (287.67 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 2.3013 mL 11.5067 mL 23.0134 mL
5 mM 0.4603 mL 2.3013 mL 4.6027 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

  • Dilution Calculator

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

Mass
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Concentration
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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)

V1

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Concentration (final)

C2

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Volume (final)

V2

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    90% Corn Oil

    Solubility: ≥ 20.83 mg/mL (47.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 20.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (208.3 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.79 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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

Purity: 99.97%

COA (253 KB) HNMR (141 KB) RP-HPLC (246 KB)

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 2.3013 mL 11.5067 mL 23.0134 mL 57.5334 mL
5 mM 0.4603 mL 2.3013 mL 4.6027 mL 11.5067 mL
10 mM 0.2301 mL 1.1507 mL 2.3013 mL 5.7533 mL
15 mM 0.1534 mL 0.7671 mL 1.5342 mL 3.8356 mL
20 mM 0.1151 mL 0.5753 mL 1.1507 mL 2.8767 mL
25 mM 0.0921 mL 0.4603 mL 0.9205 mL 2.3013 mL
30 mM 0.0767 mL 0.3836 mL 0.7671 mL 1.9178 mL
40 mM 0.0575 mL 0.2877 mL 0.5753 mL 1.4383 mL
50 mM 0.0460 mL 0.2301 mL 0.4603 mL 1.1507 mL
60 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9589 mL
80 mM 0.0288 mL 0.1438 mL 0.2877 mL 0.7192 mL
100 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
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CDK12-IN-E9 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:

CDK12-IN-E92020052-55-3CDKCyclin dependent kinaseCDK9CDK12antiproliferativeABCpyrazollopyridinephosphorylatedRNAPIIMYCMCL1Cys1039Inhibitorinhibitorinhibit

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