CDK9-IN-40
CDK9-IN-40 is a potent and orally active CDK9 inhibitor with an IC50 of 5.5 nM. CDK9-IN-40 shows high selectivity for CDK9 versus CDK1, CDK2, CDK4, and CDK6, respectively. CDK9-IN-40 can arrest cell cycle, induce cell apoptosis and inhibit tumor growth. CDK9-IN-40 exhibits strong anti-cancer activity.
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- Formule: C21H26N8S
- Masse moléculaire:422.55
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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
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Activité biologique
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CDK9 5.5 nM (IC50) |
CDK9-IN-40 (Compound 8e) (1.0 μM, 48 h) exhibits the highest inhibitory activities against CDK9 (99% inhibition, IC50 = 5.5 nM) and shows over 180 and 75-fold selectivity for CDK9 versus CDK1 and CDK2, respectively[1].
CDK9-IN-40 (1.8 μM-3.0 μM, 48 h) possesses remarkable cell growth inhibitory activity toward HeLa, A549, HCT116, and MCF-7 cells, which are greater or similar with ZK304709[1].
CDK9-IN-40 (1 μM-4 μM, 24 h) can cause the G2/M phase arrest and induce cell apoptosis in HCT116 cells in a concentration-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:HeLa, A549, HCT116, MCF-7, HEK293, LO2
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Concentration:1 μM
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Incubation Time:48 h
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Result:Offered the best CDK9 inhibitory activities (IC50 = 5.5 nM), being comparable to that of ZK304709 (IC50 = 5.0 nM) and higher than AZD5438 (IC50 = 18.0 nM).
Didn’t demonstrate obvious cytotoxic activity against two non-tumoural cells HEK-293 and LO2 (IC50 = 50 μM).
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Cell Line:HCT116
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Concentration:1.0 μM, 2.0 μM, 4.0 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent G2/M phase arrest (14.71%, 18.16%, and 24.81% respectively).
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Cell Line:HCT116
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Concentration:1.0 μM, 2.0 μM, 4.0 μM
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Incubation Time:24 h
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Result:Induced total apoptosis rates of 10.08%, 16.43%, and 33.70% with the rate of 1.0, 2.0 and 4.0 μM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old pathogen-free male Balb/c-nu mice were used to establish HCT116 xenograft models [1]
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Dosage:30 mg/kg, 60 mg/kg
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Administration:Oral gavage (PO); Once daily; for 7 days; 4 days after cell injection
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Result:Exhibited potent antitumor effects, suppressing tumor growth by 59.2% at a dose of 60 mg/kg per day.
Chemical Information
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Masse moléculaire 422.55
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Formule C21H26N8S
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SMILES
CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC(N4CCC5=C(SC(N)=N5)C4)=CC=N3
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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-40 Related Classifications
HY-176736 Related Classifications
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