上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
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 Chemical Structure
CAS No. : 2580938-58-3
规格 |
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是否有货 |
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100 mg |
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询价 |
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250 mg |
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询价 |
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500 mg |
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询价 |
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* Please select Quantity before adding items.
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].
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IC50 & Target[1] |
HDAC1
6.4 nM (IC50)
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HDAC2
0.25 nM (IC50)
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HDAC3
45 nM (IC50)
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HDAC6
>1000 nM (IC50)
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HDAC8
>1000 nM (IC50)
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CDK1
8.63 nM (IC50)
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CDK2
0.30 μM (IC50)
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CDK4
>1000 nM (IC50)
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CDK6
>1000 nM (IC50)
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CDK7
>1000 nM (IC50)
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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. |
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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. |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献 |
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