Art. -Nr.: HY-148561

CDK8-IN-12

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CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a K_i of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with K_is of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent.

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Reinheit: 99.74%
CAS. Nr.: 2613307-67-6
Formel: C₂₁H₂₀ClN₃O₂
Molecular Weight:381.86

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CDK8-IN-12 Chemical Structure

CAS. Nr.: 2613307-67-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK8

14 nM (Ki)

GSK-3α

13 nM (Ki)

GSK-3β

4 nM (Ki)

PKCθ

109 nM (Ki)

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle GSK-3 Isoform-spezifische Produkte anzeigen :

Alle PKC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	21.43 μM Compound: 38	Growth inhibition human A2780 cells after 72 hrs by resazurin or MTT assay Growth inhibition human A2780 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
COLO 205	GI₅₀	>50 μM Compound: 38	Growth inhibition human COLO 205 cells after 72 hrs by resazurin or MTT assay Growth inhibition human COLO 205 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
HCT-116	GI₅₀	40.55 μM Compound: 38	Growth inhibition human HCT-116 cells after 72 hrs by resazurin or MTT assay Growth inhibition human HCT-116 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
HL-60	GI₅₀	35.31 μM Compound: 38	Growth inhibition human HL-60 cells after 72 hrs by resazurin or MTT assay Growth inhibition human HL-60 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
HT-29	GI₅₀	44.25 μM Compound: 38	Growth inhibition human HT-29 cells after 72 hrs by resazurin or MTT assay Growth inhibition human HT-29 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
Kasumi 1	GI₅₀	>50 μM Compound: 38	Growth inhibition human Kasumi-1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human Kasumi-1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
KG-1	GI₅₀	7.13 μM Compound: 38	Growth inhibition human KG-1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human KG-1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
KG-1a	GI₅₀	19.55 μM Compound: 38	Growth inhibition human KG-1a cells after 72 hrs by resazurin or MTT assay Growth inhibition human KG-1a cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MCF7	GI₅₀	>50 μM Compound: 38	Growth inhibition human MCF7 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MCF7 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MDA-MB-231	GI₅₀	40.71 μM Compound: 38	Growth inhibition human MDA-MB-231 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MDA-MB-231 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MDA-MB-453	GI₅₀	23.32 μM Compound: 38	Growth inhibition human MDA-MB-453 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MDA-MB-453 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MOLM-13	GI₅₀	6.18 μM Compound: 38	Growth inhibition human MOLM-13 cells after 72 hrs by resazurin or MTT assay Growth inhibition human MOLM-13 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
MV4-11	GI₅₀	0.36 μM Compound: 38	Growth inhibition of human MV4-11 cells after 72 hrs by resazurin staining based assay Growth inhibition of human MV4-11 cells after 72 hrs by resazurin staining based assay	[PMID: 33571827]
NB-4	GI₅₀	40.8 μM Compound: 38	Growth inhibition human NB4 cells after 72 hrs by resazurin or MTT assay Growth inhibition human NB4 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
PANC-1	GI₅₀	>50 μM Compound: 38	Growth inhibition human PANC-1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human PANC-1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
T47D	GI₅₀	16.18 μM Compound: 38	Growth inhibition human T47D cells after 72 hrs by resazurin or MTT assay Growth inhibition human T47D cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
THP-1	GI₅₀	>50 μM Compound: 38	Growth inhibition human THP1 cells after 72 hrs by resazurin or MTT assay Growth inhibition human THP1 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
U-937	GI₅₀	1.36 μM Compound: 38	Growth inhibition human U-937 cells after 72 hrs by resazurin or MTT assay Growth inhibition human U-937 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]
WI-38	GI₅₀	48.05 μM Compound: 38	Growth inhibition human WI38 cells after 72 hrs by resazurin or MTT assay Growth inhibition human WI38 cells after 72 hrs by resazurin or MTT assay	[PMID: 33571827]

In Vitro

CDK8-IN-12 (compound 38) selectively inhibits the proliferation of MV4-11 acute myeloid leukaemia cells with a GI₅₀ of 0.36 μM^[1].
CDK8-IN-12 (0.36, 0.72 μM; 2 hours) significantly reduces the phosphorylation of serine 727 on STAT1^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.36, 0.72 μM
Incubation Time:

2 hours
Result:

Significantly reduced the phosphorylation of serine 727 on STAT1 at concentrations of their respective 1× GI50 values, but barely affected the level of total STAT1.

In Vivo

CDK8-IN-12 (compound 38; IV; 5 mg/kg for rat and 2 mg/kg for mouse) has a T_1/2 of 0.9 hours and 0.34 hours for rat and mouse, respectively^[1].
Pharmacokinetic Parameters of CDK8-IN-12 ^[1].

	IV (Rat 5 mg/kg)	PO (Rat 20 mg/kg)	IV (Mouse 2 mg/kg)	PO (Mouse 10 mg/kg)
T_max (h)	0.04	2.75	0.04	0.42
C_max (μM)	14.4	2.77	3.44	5.01
AUC_0-24 (μM∗h)	9.7	14.6	1.39	2.30
T_1/2 (ng/mL)	0.9	2.24	0.34	1.11
CL (L/h∗kg)	1.39		3.78
V_ss (L/kg)	1.11		1.99
F (%)		38		33

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

Chemical Information

CAS. Nr. 2613307-67-6
Appearance Solid
Molecular Weight 381.86
Formel C₂₁H₂₀ClN₃O₂
Color Off-white to light yellow
SMILES

O=C1NCCC12CCN(C3=C(C4=CC5=CC=CC=C5O4)C=NC=C3Cl)CC2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (174.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6188 mL

13.0938 mL

26.1876 mL

5 mM

0.5238 mL

2.6188 mL

5.2375 mL

10 mM

0.2619 mL

1.3094 mL

2.6188 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (6.55 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (6.55 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mingfeng Yu, et al. Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. Eur J Med Chem. 2021 Mar 15;214:113248. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.6188 mL	13.0938 mL	26.1876 mL	65.4690 mL
	5 mM	0.5238 mL	2.6188 mL	5.2375 mL	13.0938 mL
	10 mM	0.2619 mL	1.3094 mL	2.6188 mL	6.5469 mL
	15 mM	0.1746 mL	0.8729 mL	1.7458 mL	4.3646 mL
	20 mM	0.1309 mL	0.6547 mL	1.3094 mL	3.2735 mL
	25 mM	0.1048 mL	0.5238 mL	1.0475 mL	2.6188 mL
	30 mM	0.0873 mL	0.4365 mL	0.8729 mL	2.1823 mL
	40 mM	0.0655 mL	0.3273 mL	0.6547 mL	1.6367 mL
	50 mM	0.0524 mL	0.2619 mL	0.5238 mL	1.3094 mL
	60 mM	0.0436 mL	0.2182 mL	0.4365 mL	1.0912 mL
	80 mM	0.0327 mL	0.1637 mL	0.3273 mL	0.8184 mL
	100 mM	0.0262 mL	0.1309 mL	0.2619 mL	0.6547 mL

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CDK8-IN-12

Cell Cycle/DNA Damage Compound Library

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Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Alle GSK-3 Isoform-spezifische Produkte anzeigen

Alle PKC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CDK8-IN-12 Related Classifications

Art. -Nr.: HY-148561