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

CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.

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

CDK12-IN-3 Chemical Structure

CDK12-IN-3 Chemical Structure

CAS No. : 2220184-50-7

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
5 mg USD 400 In-stock
10 mg USD 650 In-stock
25 mg USD 1380 In-stock
50 mg USD 2290 In-stock
100 mg USD 3890 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.

IC50 & Target[1]

CDK12

491 nM (IC50)

In Vitro

CDK12-IN-3 is a highly selective CDK12 inhibitor. CDK12-IN-3 (0.1 μM) shows potent inhibition of phosphorylation of Ser2 on the CTD repeat domain of RNA Pol II as well as growth inhibition of OV90 cells and acute cytotoxicity to THP1 cells.[1].

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

Molecular Weight

470.52

Formula

C23H28F2N8O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)N1C2=NC(N3CCCC[C@H]3CCO)=NC(NCC4=NC5=C(C(F)=C(F)C=C5)N4)=C2N=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (531.33 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 2.1253 mL 10.6265 mL 21.2531 mL
5 mM 0.4251 mL 2.1253 mL 4.2506 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
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

×
Volume (start)

V1

=
Concentration (final)

C2

×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.33 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (23.3 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% Corn Oil

    Solubility: ≥ 2.33 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.33 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 (23.3 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1253 mL 10.6265 mL 21.2531 mL 53.1327 mL
5 mM 0.4251 mL 2.1253 mL 4.2506 mL 10.6265 mL
10 mM 0.2125 mL 1.0627 mL 2.1253 mL 5.3133 mL
15 mM 0.1417 mL 0.7084 mL 1.4169 mL 3.5422 mL
20 mM 0.1063 mL 0.5313 mL 1.0627 mL 2.6566 mL
25 mM 0.0850 mL 0.4251 mL 0.8501 mL 2.1253 mL
30 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7711 mL
40 mM 0.0531 mL 0.2657 mL 0.5313 mL 1.3283 mL
50 mM 0.0425 mL 0.2125 mL 0.4251 mL 1.0627 mL
60 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
80 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.6642 mL
100 mM 0.0213 mL 0.1063 mL 0.2125 mL 0.5313 mL
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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.

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Product Name:
CDK12-IN-3
Cat. No.:
HY-112261
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