CDK9-IN-33
CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity.
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- Formule: C23H31N7O2
- Masse moléculaire:437.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CDK9 17.44 nM (IC50) |
CDK7 160 nM (IC50) |
CDK2 316.30 nM (IC50) |
CDK4 1771.00 nM (IC50) |
CDK6 >10000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| 4T1 | IC50 |
20.08 nM
Compound: C35
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Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| BT-549 | IC50 |
5.61 nM
Compound: C35
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Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| MDA-MB-231 | IC50 |
5.9 nM
Compound: C35
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Inhibition of cell viability in human MDA-MB-231 cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in human MDA-MB-231 cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| MDA-MB-468 | IC50 |
10.05 nM
Compound: C35
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Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
| MM1.S | IC50 |
2438 nM
Compound: C35
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Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay
Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay
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[PMID: 38885173] |
CDK9-IN-33 (compound C35) (0, 0.01, 0.1, 1 µM; 24 h) decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1 and increases the expression of cleaved PARP[1].
CDK9-IN-33 (0, 0.01, 0.1, 1 µM) decreases the mRNA expression levels of the MCL1 gene[1].
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CDK9-IN-33 (0, 0.01, 0.1, 1 µM; 72 h) induces apoptosis in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells
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Concentration:
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Incubation Time:4 days
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Result:Showed antiproliferation potential for MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells with IC50 values of 5.9, 10.05, 5.61, 20.08, 8.98, 24.38 nM, respectively.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 0.01, 0.1, 1 µM
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Incubation Time:24 h
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Result:Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 0.01, 0.1, 1 µM
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Incubation Time:24 h
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Result:Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.
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Cell Line:4T1 cells
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Concentration:0, 0.01, 0.1, 1 µM
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Incubation Time:72 h
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Result:Induced apoptosis in a dose-dependent manner.
Pharmacokinetic Parameters (male ICR mice; p.o. 20.0 mg/kg, i.v. 5.0 mg/kg; )[1].
| Cmpd | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (h·ng/mL) | AUCt–∞ (h·ng/mL) | CL (mL/min/kg) | MRT0–∞ (h) | Vss (mL/kg) | F (%) |
| C35 (p.o.) | 0.68 | 0.5 | 2867 | 4349 | 4350 | - | 1.43 | - | 68.9 |
| C35 (i.v.) | 0.36 | - | - | 1578 | 1578 | 52.9 | 0.33 | 1033 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 437.54
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Formule C23H31N7O2
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SMILES
CC(C1=C2N=C(N=C(N2N=C1)NCC3=CC=C(C=C3)NC(CC)=O)NC4CCOCC4)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK9-IN-33 Related Classifications
HY-162619 Related Classifications
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