2. Cell Cycle/DNA Damage
  3. CDK
  4. CCT-251921

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.

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

CCT-251921 Chemical Structure

CCT-251921 Chemical Structure

CAS No. : 1607837-31-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 260 In-stock
Solution
10 mM * 1 mL in DMSO USD 260 In-stock
Solid
1 mg USD 108 In-stock
5 mg USD 288 In-stock
10 mg USD 420 In-stock
25 mg USD 840 In-stock
50 mg USD 1140 In-stock
100 mg USD 1620 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

CCT-251921 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CCT-251921

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

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.

IC50 & Target[1]

CDK8

2.3 nM (IC50)

CDK19

2.6 nM (IC50)

In Vitro

CCT-251921 has acceptable aqueous solubility and demonstrates minimal activity when tested in a panel of 55 receptors, ion channels, and enzymes at 1 μM and in a panel of 279 kinases; weak inhibition of CYPs is observed. CCT-251921 demonstrates potent inhibition of reporter-based readouts measuring basal WNT pathway activity in human cancer cell lines that have constitutively activated WNT pathway signaling: LS174T (β-catenin mutant), SW480 and Colo205 (APC mutant) or PA-1 human teratocarcinoma cells that are WNT ligand dependent[1].

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

CCT-251921 Related Antibodies
In Vivo

CCT-251921 shows improved oral pharmacokinetics and pharmaceutical properties in order to facilitate further evaluation of CDK8/19 pharmacology and progression into preclinical efficacy and safety studies. In APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduces mice tumor weight (54.2%) at day 15. The inhibition of STAT1SER727 phosphorylation is maintained for more than 6 h after the last dose[1].

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

410.90

Formula

C21H23ClN6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NCCC12CCN(C3=C(Cl)C(N)=NC=C3C4=CC5=C(N(C)N=C5)C=C4)CC2
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 : 25 mg/mL (60.84 mM; ultrasonic and warming and heat to 60°C; 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 2.4337 mL 12.1684 mL 24.3368 mL
5 mM 0.4867 mL 2.4337 mL 4.8674 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
×
Volume
×
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: ≥ 2.5 mg/mL (6.08 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.08 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:

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: 99.01%

COA (255 KB) LCMS (106 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

7dF3 cells are treated with CCT-251921 ranging in final concentration from 90 μM to 0.3 nM. After 2 h of further incubation, β-oestradiol is added to a final concentration of 10 μM. The cells are incubated and then 25 μL of luciferase reagent is added and mixed. After leaving the plate for 60 min at room temperature, luminescence is read on a plate luminescence reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Animals are dosed orally by gavage every 24 h at 0.1 mL per 10 g body weight. Tumors are measured three times weekly by Vernier calipers and body weights recorded. At the end of the study, animals are culled at intervals: 3 control and 3 treated at 1, 2, 6, and 24 h after the final dose. Heparinized blood is collected by cardiac puncture, spun, and plasma snap frozen for analysis of compound exposure. Tumors are excised, weighed and samples snap frozen for compound quantification and PD analyses. The 30 mg/kg q.d. schedule is well tolerated with no significant body weight loss. Tumor growth is significantly inhibited[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 2.4337 mL 12.1684 mL 24.3368 mL 60.8421 mL
5 mM 0.4867 mL 2.4337 mL 4.8674 mL 12.1684 mL
10 mM 0.2434 mL 1.2168 mL 2.4337 mL 6.0842 mL
15 mM 0.1622 mL 0.8112 mL 1.6225 mL 4.0561 mL
20 mM 0.1217 mL 0.6084 mL 1.2168 mL 3.0421 mL
25 mM 0.0973 mL 0.4867 mL 0.9735 mL 2.4337 mL
30 mM 0.0811 mL 0.4056 mL 0.8112 mL 2.0281 mL
40 mM 0.0608 mL 0.3042 mL 0.6084 mL 1.5211 mL
50 mM 0.0487 mL 0.2434 mL 0.4867 mL 1.2168 mL
60 mM 0.0406 mL 0.2028 mL 0.4056 mL 1.0140 mL
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CCT-251921 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:

CCT-2519211607837-31-9CCT251921CCT 251921CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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