CDK/HDAC-IN-2

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CDK/HDAC-IN-2 

CDK/HDAC-IN-2 是一种有效的 HDAC/CDK 双重抑制剂，对于 HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, IC50 分别为 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM。CDK/HDAC-IN-2 显示出优异的抗增殖活性。CDK/HDAC-IN-2 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G2/M 期。CDK/HDAC-IN-2 显示出强大的抗肿瘤功效。

CDK/HDAC-IN-2

CDK/HDAC-IN-2 Chemical Structure

CAS No. : 2580938-58-3

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生物活性

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[1].

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)

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

体内研究
(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.
t1/2 (h) 2.61
Tmax (h) 2.00
Cmax (h) 7570
AUC0-∞ (ng h/mL) 30700
MRT0-∞ (ng h/mL) 3.31
F (%) 63.6

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

Shanghai Jinpan Biotech Co Ltd 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.

分子量

523.37

Formula

C25H20Cl2N6O3
CAS 号

2580938-58-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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.

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