Art. -Nr.: HY-112460

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CDK2-IN-3

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CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an IC₅₀ of 60 nM.

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Reinheit: 95.12%
CAS. Nr.: 222035-13-4
Formel: C₁₄H₁₁BrN₄O₃S
Molecular Weight:395.23

Speicherung:

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

CDK2-IN-3 Chemical Structure

CAS. Nr.: 222035-13-4

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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

CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an IC₅₀ of 60 nM^[1].

IC₅₀ & Target^[1]

CDK2

60 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.031 μM Compound: Fig.4B, R5C1	Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.738 μM Compound: Fig.4B, R5C1	Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	1.1 μM Compound: Fig.4B, R5C1	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	1.3 μM Compound: Fig.4B, R5C1	Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	19.7 μM Compound: Fig.4B, R5C1	Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	2.8 μM Compound: Fig.4B, R5C1	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]

In Vitro

CDK2-IN-3 (12 µM, 24 hour) significantly protects CCL64 mink lung epithelial cells from cytotoxic damage induced by various chemotherapy drugs (Taxol, Etoposide (HY-13629), Cisplatin (HY-17394), 5-FU (HY-90006), Doxorubicin (HY-15142A))^[1].
CDK2-IN-3 (7.5 µM, 6 hours) significantly blocks G1/S transition and inhibits DNA synthesis in human diploid fibroblasts^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

Human diploid fibroblasts (HDFs)
Concentration:

7.5 µM
Incubation Time:

6 h
Result:

Blocked G1/S transition, significantly reduced DNA synthesis (decreased percentage of BrdU-positive cells).

In Vivo

CDK2-IN-3 (2.5-250 µg, topical application, once daily, for 1 week) significantly reduces the incidence of alopecia in neonatal rat model induced by the combination of cyclophosphamide (HY-17420) and doxorubicin (HY-15142A)^[1].

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

Animal Model:

Cyclophosphamide (HY-17420)-Doxorubicin (HY-15142A) combination chemotherapy-induced alopecia neonatal Sprague-Dawley rat model (13 days)
Dosage:

2.5-250 µg
Administration:

Topical application, once daily for 1 week
Result:

Effectively prevented alopecia in 50% of rats and provided partial protection in an additional 20%.

Chemical Information

CAS. Nr. 222035-13-4
Appearance Solid
Molecular Weight 395.23
Formel C₁₄H₁₁BrN₄O₃S
Color Light yellow to yellow
SMILES

O=S(C1=CC=C(N/N=C2C(NC3=C\2C=C(Br)C=C3)=O)C=C1)(N)=O
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 : 100 mg/mL (253.02 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

2.5302 mL

12.6509 mL

25.3017 mL

5 mM

0.5060 mL

2.5302 mL

5.0603 mL

10 mM

0.2530 mL

1.2651 mL

2.5302 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 (6.33 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.

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 (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. S T Davis, et al. Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors. Science. 2001 Jan 5;291(5501):134-7. [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	2.5302 mL	12.6509 mL	25.3017 mL	63.2543 mL
	5 mM	0.5060 mL	2.5302 mL	5.0603 mL	12.6509 mL
	10 mM	0.2530 mL	1.2651 mL	2.5302 mL	6.3254 mL
	15 mM	0.1687 mL	0.8434 mL	1.6868 mL	4.2170 mL
	20 mM	0.1265 mL	0.6325 mL	1.2651 mL	3.1627 mL
	25 mM	0.1012 mL	0.5060 mL	1.0121 mL	2.5302 mL
	30 mM	0.0843 mL	0.4217 mL	0.8434 mL	2.1085 mL
	40 mM	0.0633 mL	0.3163 mL	0.6325 mL	1.5814 mL
	50 mM	0.0506 mL	0.2530 mL	0.5060 mL	1.2651 mL
	60 mM	0.0422 mL	0.2108 mL	0.4217 mL	1.0542 mL
	80 mM	0.0316 mL	0.1581 mL	0.3163 mL	0.7907 mL
	100 mM	0.0253 mL	0.1265 mL	0.2530 mL	0.6325 mL

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CDK2-IN-3

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase 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

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CDK2-IN-3

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase 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

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CDK2-IN-3 Related Classifications

HY-112460 Related Classifications