CDK6-IN-2
CDK6-IN-2 is a CDK6 covalent inhibitor with an IC50 of 0.013 μM. CDK6-IN-2 inhibits the proliferation and migration of triple-negative breast cancer cells, and induces cell cycle arrest and apoptosis. CDK6-IN-2 induces ROS accumulation and mitochondrial damage through cellular metabolic reprogramming. CDK6-IN-2 exhibits anti-tumor activity and can be used for the research of triple-negative breast cancer.
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- Formule: C24H29BrN6O3
- Masse moléculaire:529.43
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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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CDK6 0.013 μM (IC50) |
Caspase 3 |
CDK6-IN-2 (compound C32) (72 h) selectively inhibits the viability of TNBC and BRCA1-mutant breast cancer cells with an IC50 value ≤ 0.08 μM, while exhibits low activity against normal mammary epithelial cells and ER-positive breast cancer cells[1].
CDK6-IN-2 (0-0.2 μM; 0-72 h) potently inhibits the proliferation and migration of MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells, and induces apoptosis, cell cycle arrest, and intracellular ROS accumulation[1].
CDK6-IN-2 (0-0.20 μM; 72 h) induces mitochondrial damage and dysfunction, including reduced membrane potential and structural abnormalities, in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells[1].
CDK6-IN-2 (0-0.20 μM; 72 h) inhibits autophagic flux and degradation processes in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells, which is evidenced by the co-accumulation of LC3II and P62 proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Triple-negative breast cancer (TNBC) lines MDA-MB-231, MDA-MB-468, BT-549; BRCA1-mutant line MDA-MB-436; ER-positive line MCF-7; normal mammary epithelial line MCF-10A
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Concentration:/
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Incubation Time:72 h
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Result:Selectively inhibited the viability of TNBC and BRCA1-mutant breast cancer cells with IC50 values of 0.06 μM (MDA-MB-231), 0.08 μM (MDA-MB-468), 0.04 μM (BT-549), and 0.06 μM (MDA-MB-436).
Showed reduced activity against non-TNBC cells with IC50 = 0.39 μM (MCF-7), 2.30 μM (MCF-10A).
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Cell Line:TNBC cell lines MDA-MB-231 and BT-549
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Concentration:MDA-MB-231: 0.1, 0.15, 0.2 μM; BT-549: 0.08, 0.12, 0.16 μM
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Incubation Time:72 h
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Result:Concentration-dependently reduced the number of EdU-positive proliferating cells in both TNBC lines.
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Cell Line:TNBC cell line MDA-MB-231
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Concentration:0.10, 0.15, 0.20 μM
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Incubation Time:72 h
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Result:Induced a concentration-dependent S-phase cell cycle arrest, with the proportion of S-phase cells increasing from 35.91% (control) to 40.68% (0.10 μM), 48.31% (0.15 μM), and 55.9% (0.20 μM), while the proportion of G0/G1-phase cells decreased correspondingly.
| Species | Dose | Route | C0 | AUC0-t | AUC0-∞ | T1/2 | Vd/F | CL/F |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 772.60 ng/mL | 82.75 ng·h/mL | 93.80 ng·h/mL | 0.59 h | 13.09 L/kg | 15.46 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 4 weeks old, subcutaneous inoculation of 1×107 MDA-MB-231 cells)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 18 days
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Result:Reduced mean tumor weight to 0.68 g (10 mg/kg group) and 0.23 g (20 mg/kg group), significantly lower than the control group's 1.45 g.
Significantly down-regulated Ki67, CDK6, and RB1 positive cell counts in treated tumor tissues.
Significantly up-regulated Cleaved Caspase-3 positive cell counts in treated tumor tissues.
Caused no significant changes in mouse body weight.
Showed no pathological damage to major organs (heart, liver, spleen, lung, kidney) via H&E staining.
Chemical Information
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Masse moléculaire 529.43
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Formule C24H29BrN6O3
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SMILES
C#CC(NC(C)C(N1CCC(NC2=NC=C(C(C)=C(Br)C(N3C4CCCC4)=O)C3=N2)CC1)=O)=O
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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)
CDK6-IN-2 Related Classifications
HY-181483 Related Classifications
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