1. Cell Cycle/DNA Damage
  2. CDK
  3. Senexin C

Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability.

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

Senexin C Chemical Structure

Senexin C Chemical Structure

CAS No. : 2375554-02-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 638 In-stock
Solution
10 mM * 1 mL in DMSO USD 638 In-stock
Solid
5 mg USD 580 In-stock
10 mg USD 985 In-stock
25 mg USD 2060 In-stock
50 mg USD 3500 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability[1].

IC50 & Target[1]

CDK8/CycC

3.6 nM (IC50)

CDK19/CycC

2.9 nM (Kd)

CDK8/CycC

1.4 nM (Kd)

In Vitro

Senexin C (compound 20a) exhibits potent CDK8/19 inhibitory activity with high selectivity (IC50s of 56 and 108 nM for 293-NFκB-Luc and MV4-11-Luc cells, respectively)[1].
Senexin C (2 µM) shows potency in different kinase assays (IC50= 3.6 nM for CD8/CycC, Kd=1.4 nM for CD8/CycC, Kd=2.9 nM for CDK19/CycC)[1].
Senexin C (1 µM, 3 h) shows inhibition on CDK8/19 dependent cellular gene expression[1].

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

RT-PCR[1]

Cell Line: 293 cells
Concentration: 1 µM
Incubation Time: 3 h
Result: Showed inhibition on CDK8/19 dependent cellular gene expression.
In Vivo

Senexin C (2.5 mg/kg, i.v.; 100 mg/kg, p.o.) shows good oral bioavailability[1].
Senexin C (40 mg/kg; p.o.; twice daily for 4 weeks) suppresses the systemic growth of MV4-11 AML with good tolerability[1]. Pharmacokinetic Parameters of Senexin C in eight-week-old female Balb/c mice[1].

parameters iv (2.5 mg/kg) po (100 mg/kg)
plasma tumor plasma tumor
C0 (μg/mL) 503
Kel (h-1) 0.93 0.06 0.2 0.1
T1/2 (h) 0.75 12.1 3.53 7.27
Tmax (h) 0.58 12 12
Cmax (ng/mL or ng/g) 488 144 5728
AUC0-24 h (ng x h/ml or ng x h/g) 331 6408 2182 88,600
F% 16.5% 34.6%
Eight-week-old female Balb/c mice ( CT26 tumor mode), 2.5 mg/kg, i.v.(2.5 mg/mL Senexin C solution in 5% dextrose); 100 mg/kg, p.o.(10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle)[1].

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

Animal Model: eight-week-old female Balb/c mice ( CT26 tumor mode)[1]
Dosage: 2.5 mg/kg (10 mL/kg of 2.5 mg/mL Senexin C solution in 5% dextrose), 100 mg/kg (10 mL/kg of 10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle)
Administration: 2.5 mg/kg, i.v.; 100 mg/kg, p.o.
Result: Showed good oral bioavailability.
Animal Model: eight-week-old female NSG mice ( AML model)[1]
Dosage: 40 mg/kg
Administration: p.o.; twice daily, 4 weeks
Result: Suppressed the systemic growth of MV4-11 AML with good tolerability.
Molecular Weight

449.55

Formula

C28H27N5O

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=CC=C2N=CC=C(NCCC3=CC=C4C=C(C(N5CCN(C)CC5)=O)C=CC4=C3)C2=C1

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 (74.14 mM; ultrasonic and warming and heat to 160°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 2.2244 mL 11.1222 mL 22.2445 mL
5 mM 0.4449 mL 2.2244 mL 4.4489 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
=
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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.56 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:

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, 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 2.2244 mL 11.1222 mL 22.2445 mL 55.6112 mL
5 mM 0.4449 mL 2.2244 mL 4.4489 mL 11.1222 mL
10 mM 0.2224 mL 1.1122 mL 2.2244 mL 5.5611 mL
15 mM 0.1483 mL 0.7415 mL 1.4830 mL 3.7074 mL
20 mM 0.1112 mL 0.5561 mL 1.1122 mL 2.7806 mL
25 mM 0.0890 mL 0.4449 mL 0.8898 mL 2.2244 mL
30 mM 0.0741 mL 0.3707 mL 0.7415 mL 1.8537 mL
40 mM 0.0556 mL 0.2781 mL 0.5561 mL 1.3903 mL
50 mM 0.0445 mL 0.2224 mL 0.4449 mL 1.1122 mL
60 mM 0.0371 mL 0.1854 mL 0.3707 mL 0.9269 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Senexin C 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Senexin C
Cat. No.:
HY-143889
Quantity:
MCE Japan Authorized Agent: