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

CCT-251921 

Cat. No.: HY-19984 Purity: 99.77%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 260 In-stock
Estimated Time of Arrival: December 31
1 mg USD 108 In-stock
Estimated Time of Arrival: December 31
5 mg USD 288 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
25 mg USD 840 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1620 In-stock
Estimated Time of Arrival: December 31
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
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  • Protocol

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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].

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

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].

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

Molecular Weight

410.90

Formula

C₂₁H₂₃ClN₆O

CAS No.

1607837-31-9

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (81.11 mM; Need ultrasonic)

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
10 mM 0.2434 mL 1.2168 mL 2.4337 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: 99.77%

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Keywords:

CCT-251921CCT251921CCT 251921CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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Product Name:
CCT-251921
Cat. No.:
HY-19984
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