country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-146276

Copy Link Print Information

CDK/HDAC-IN-2

CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC₅₀ of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2580938-58-3
Formel: C₂₅H₂₀Cl₂N₆O₃
Molecular Weight:523.37

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

CDK/HDAC-IN-2 Chemical Structure

CAS. Nr.: 2580938-58-3

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC1

6.4 nM (IC₅₀)

HDAC2

0.25 nM (IC₅₀)

HDAC3

45 nM (IC₅₀)

HDAC6

>1000 nM (IC₅₀)

HDAC8

>1000 nM (IC₅₀)

CDK1

8.63 nM (IC₅₀)

CDK2

0.30 μM (IC₅₀)

CDK4

>1000 nM (IC₅₀)

CDK6

>1000 nM (IC₅₀)

CDK7

>1000 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1.2 μM Compound: 7c	Antiproliferative activity against human A375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31991336]
HCT-116	IC₅₀	0.71 μM Compound: 7c	Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31991336]
HeLa	IC₅₀	1.83 μM Compound: 7c	Antiproliferative activity against human Hela cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Hela cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31991336]
NCI-H460	IC₅₀	4.19 μM Compound: 7c	Antiproliferative activity against human H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31991336]
SMMC-7721	IC₅₀	7.76 μM Compound: 7c	Antiproliferative activity against human SMMC7721 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SMMC7721 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31991336]

In Vitro

CDK/HDAC-IN-2 (compound 7c) shows antiproliferative activity with IC₅₀s of 0.71, 1.20, 1.83, 4.19, 7.76, 4.47 µM for HCT116, A375, Hela, H460, SMMC7721, NIH 3T3 cells, respectively^[1].
CDK/HDAC-IN-2 (24 h) shows anti-migration ability in A375 and H460 cells^[1].
CDK/HDAC-IN-2 (0.5, 1, 2 µM) induces apoptosis and cell cycle arrest at G2/M phase^[1].
CDK/HDAC-IN-2 accelerates intracellular ROS accumulation, leading to cancer cell death^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

A375, HCT116, H460, Hela cells
Concentration:

0.5, 1, 2 µM
Incubation Time:

24 h
Result:

Induced cell cycle arrest at G2/M phase.

Apoptosis Analysis^[1]

Cell Line:

A375, HCT116, H460, Hela cells
Concentration:

0.5, 1, 2 µM
Incubation Time:

48 h
Result:

Induced cell apoptosis with the apoptosis rates of A375, HCT116 cells of 97.22%, 60.6%, respectively.

In Vivo

CDK/HDAC-IN-2 (12.5, 25 mg/kg; IP; once daily for 21 days) shows antitumor efficacy in the HCT116 xenograft model (TGI= 51.0%)^[1].
Pharmacokinetic Parameters of CDK/HDAC-IN-2 in ICR male mice^[1].

compound	7c
Dose (mg/kg)	20
administration	i.p.
t_1/2 (h)	2.61
T_max (h)	2.00
C_max (h)	7570
AUC_0-∞ (ng h/mL)	30700
MRT_0-∞ (ng h/mL)	3.31
F (%)	63.6

ICR male mice; 20 mg/kg, i.p.^[1].

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

Animal Model:

ICR male mice^[1]
Dosage:

20 mg/kg
Administration:

IP
Result:

Showed good Pharmacokinetic parameters with bioavailability of F= 63.6%.

Animal Model:

5-6 weeks, BALB/c female mice (HCT116 xenograft nude mice models)^[1]
Dosage:

12.5, 25 mg/kg
Administration:

IP, once daily for 21 days
Result:

Effectively inhibited the growth of HCT116 xenograft tumors tumor growth inhibitions (TGI) at 12.5 and 25 mg/kg of 37.0% and 51.0%, respectively.

Chemical Information

CAS. Nr. 2580938-58-3
Molecular Weight 523.37
Formel C₂₅H₂₀Cl₂N₆O₃
SMILES

NC1=CC=CC=C1NC(C2=CC=C(C=C2)CNC(C3=NNC=C3NC(C4=C(C=CC=C4Cl)Cl)=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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]. Cheng C, et al. Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity. Eur J Med Chem. 2020 Mar 1;189:112073. [Content Brief]

Calculators

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)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

CDK/HDAC-IN-2

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CDK/HDAC-IN-2 Related Classifications

HY-146276 Related Classifications