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.
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- CAS No.: 2580938-58-3
- 화학식: C25H20Cl2N6O3
- 분자량:523.37
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
1.2 μM
Compound: 7c
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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
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[PMID: 31991336] |
| HCT-116 | IC50 |
0.71 μM
Compound: 7c
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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
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[PMID: 31991336] |
| HeLa | IC50 |
1.83 μM
Compound: 7c
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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
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[PMID: 31991336] |
| NCI-H460 | IC50 |
4.19 μM
Compound: 7c
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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
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[PMID: 31991336] |
| SMMC-7721 | IC50 |
7.76 μM
Compound: 7c
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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
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[PMID: 31991336] |
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.
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Cell Line:A375, HCT116, H460, Hela cells
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Concentration:0.5, 1, 2 µM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at G2/M phase.
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Cell Line:A375, HCT116, H460, Hela cells
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Concentration:0.5, 1, 2 µM
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Incubation Time:48 h
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Result:Induced cell apoptosis with the apoptosis rates of A375, HCT116 cells of 97.22%, 60.6%, respectively.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR male mice[1]
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Dosage:20 mg/kg
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Administration:IP
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Result:Showed good Pharmacokinetic parameters with bioavailability of F= 63.6%.
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Animal Model:5-6 weeks, BALB/c female mice (HCT116 xenograft nude mice models)[1]
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Dosage:12.5, 25 mg/kg
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Administration:IP, once daily for 21 days
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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
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CAS No. 2580938-58-3
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분자량 523.37
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화학식 C25H20Cl2N6O3
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SMILES
NC1=CC=CC=C1NC(C2=CC=C(C=C2)CNC(C3=NNC=C3NC(C4=C(C=CC=C4Cl)Cl)=O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK/HDAC-IN-2 Related Classifications
HY-146276 Related Classifications
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