Referencia número: HY-162919

YK-2168

Revisión del cliente

Based on 1 Customer Validation

YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. YK-2168 inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses expression of CDK9-regulated genes including MYC and Mcl1, and inhibits tumor growth in CDX mice models. YK-2168 can be used for the research of cancer, such as leukemia.

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Pureza: 98.05%
No. CAS: 2571068-74-9
Fòrmula: C₁₆H₁₈ClN₅
Peso molecular:315.80

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

YK-2168 Chemical Structure

No. CAS: 2571068-74-9

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

CDK9

5.9 nM (IC₅₀)

CDK2

266.9 nM (IC₅₀)

CDK1

427.7 nM (IC₅₀)

Ver todos los productos específicos de isoformas CDK :

In Vitro

YK-2168 potently inhibits purified CDK9 enzymatic activity with an IC₅₀ of 5.9 nM, and exhibits 72.5-fold and 45.2-fold selectivity over purified CDK1 (IC₅₀ = 427.7 nM) and CDK2 (IC₅₀ = 266.9 nM), respectively^[1].
YK-2168 inhibits proliferation of MV4-11 leukemia cells with an IC₅₀ of 53.4 nM^[1].
YK-2168 30 μM) does not inhibit hERG channel activity at concentrations up to 30 μM^[1].

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

Parmacokinetics

Species	Dose	Route	V_d	CL	T_1/2	AUC_0-24
Mice^[1]	2 mg/kg	i.v.	10.2 L/kg	115 mL/min/kg	1.47 h	916 nM·h
Rat^[1]	4 mg/kg	i.v.	11.2 L/kg	52.0 mL/min/kg	3.20 h	1250 ng·h/mL
Dog^[1]	1 mg/kg	i.v.	7.62 L/kg	29.1 mL/min/kg	3.96 h	568 ng·h/mL

In Vivo

YK-2168 (5-15 mg/kg; i.v.; once weekly; 4 weeks) induces dose-dependent inhibitionof tumor growth in MV4-11 CDX mice models^[1].

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

Animal Model:

CD-1 mouse cell-derived xenograft
(CDX) model of leukemia (MV4-11) cell line^[1]
Dosage:

5, 10,15 mg/kg
Administration:

i.v.; once weekly; 4 weeks
Result:

Achieved a tumor growth inhibition (TGI) of 80% at 10 mg/kg.
Induced dose-dependent reduction of pS2-RNA Pol II CTD levels in tumor tissue.
Suppressed CDK9-regulated MYC and Mcl1 protein expression lasting up to 24 hours post-treatment.
Upregulated cleaved caspase 3 in a time-dependent manner, indicating induced apoptosis.
Showed body weight changes statistically indistinguishable from vehicle controls, indicating good safety.

Chemical Information

No. CAS 2571068-74-9
Appearance Solid
Peso molecular 315.80
Fòrmula C₁₆H₁₈ClN₅
Color Off-white to light yellow
SMILES

ClC1=CN=C(NC(C2CCNCC2)=C3)C3=C1C4=CN(C)N=C4
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (316.66 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)

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

3.1666 mL

15.8328 mL

31.6656 mL

5 mM

0.6333 mL

3.1666 mL

6.3331 mL

10 mM

0.3167 mL

1.5833 mL

3.1666 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 5 mg/mL (15.83 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

Solubility: ≥ 5 mg/mL (15.83 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (275 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Liu Y, et al. Discovery and preclinical profile of YK-2168, a differentiated selective CDK9 inhibitor in clinical development. Bioorg Med Chem Lett. 2024;112:129941. [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	3.1666 mL	15.8328 mL	31.6656 mL	79.1640 mL
	5 mM	0.6333 mL	3.1666 mL	6.3331 mL	15.8328 mL
	10 mM	0.3167 mL	1.5833 mL	3.1666 mL	7.9164 mL
	15 mM	0.2111 mL	1.0555 mL	2.1110 mL	5.2776 mL
	20 mM	0.1583 mL	0.7916 mL	1.5833 mL	3.9582 mL
	25 mM	0.1267 mL	0.6333 mL	1.2666 mL	3.1666 mL
	30 mM	0.1056 mL	0.5278 mL	1.0555 mL	2.6388 mL
	40 mM	0.0792 mL	0.3958 mL	0.7916 mL	1.9791 mL
	50 mM	0.0633 mL	0.3167 mL	0.6333 mL	1.5833 mL
	60 mM	0.0528 mL	0.2639 mL	0.5278 mL	1.3194 mL
	80 mM	0.0396 mL	0.1979 mL	0.3958 mL	0.9896 mL
	100 mM	0.0317 mL	0.1583 mL	0.3167 mL	0.7916 mL

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YK-2168

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death 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

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ver todos los productos específicos de isoformas CDK

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

YK-2168

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death 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

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ver todos los productos específicos de isoformas CDK

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

YK-2168 Related Classifications

HY-162919 Related Classifications