CDK4/6-IN-30
CDK4/6-IN-30 is a selective, orally active CDK4 and CDK6 inhibitor with IC50 values of 10 nM and 16 nM, respectively. CDK4/6-IN-30 induces cell cycle arrest at G1 phase, inhibits RB phosphorylation, and decreases c-MYC and Cyclin D1 levels. CDK4/6-IN-30 exhibits anticancer activity against breast cancer. CDK4/6-IN-30 can be used for research on breast cancer.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2699091-14-8
- 分子式: C24H26FN7O
- 分子量:447.51
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
CDK4 10 nM (IC50) |
CDK6 16 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MCF7 | GI50 |
2.698 μM
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Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
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36350721 |
| T47D | GI50 |
0.8868 μM
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Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
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36350721 |
| ZR-75-1 | GI50 |
3.202 μM
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Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
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36350721 |
| MCF-10A | GI50 |
17.65 μM
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Antiproliferative activity against human MCF 10A cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human MCF 10A cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
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36350721 |
体外実験
CDK4/6-IN-30 (Compound 42) effectively inhibits CDK6 with an IC50 of 16 nM[1].
CDK4/6-IN-30 exhibits potent inhibitory activity against CDK4 (IC50 = 10 nM) and shows high selectivity over CDK1, CDK2, CDK7, and CDK9[1].
CDK4/6-IN-30 (1.5-6 μM; 24 h) induces cell cycle arrest at G1 phase in a dose-dependent manner in both MCF-7 and T47D cells[1].
CDK4/6-IN-30 (24 h) exhibits targeted inhibition of CDK4/6 in breast cancer cells, leading to decreased RB phosphorylation and reduced c-MYC and cyclin D1 levels[1].
CDK4/6-IN-30 exhibits high stability in liver microsomes, with a t1/2 of 108 min[1].
CDK4/6-IN-30 (10 μM; 5 min) exhibits low inhibitory activity against CYP450 3A4 (12.36% inhibition at 10 μM)[1].
CDK4/6-IN-30 (72 h) significantly inhibits the proliferation of MCF-7, T47D, and ZR-75-1 breast cancer cells, while exhibiting low toxicity to normal MCF 10A cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 and T47D
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Concentration:1.5, 3, 6 μM (MCF-7); 1, 2, 4 μM (T47D)
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Incubation Time:24 h
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Result:In MCF-7 cells, increased the G1 phase population to 79.52% at 1.5 μM, 83.91% at 3 μM, and 85.27% at 6 μM.
In T47D cells, increased the G1 phase population to 83.14% at 1 μM, 85.48% at 2 μM, and 87.12% at 4 μM.
Parmacokinetics
体内実験
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 mice[1]
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Dosage:100 mg/kg and 150 mg/kg
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Administration:p.o.; once daily; 23 days
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Result:Significantly inhibited tumor growth of the MCF-7 xenograft model.
The antitumor activity improved as the dose increased, and the high dose (150 mg/kg) showed more potent antitumor activity than palbociclib (100 mg/kg).
The body weight of mice in each group increased normally.
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Animal Model:ICR mice[1]
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Dosage:1,000, 2,500, and 5,000 mg/kg
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Administration:p.o.; single administration
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Result:All mice grew normally, and no mice died even at the dosage of 5,000 mg/kg.
The weight of the main organs (heart, liver, spleen, lung, and kidney) showed no difference between the control group and the three administration groups.
HE staining showed no obvious lesions in the main organs of mice in the 5,000 mg/kg group.
化学情報
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CAS 番号 2699091-14-8
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分子量 447.51
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分子式 C24H26FN7O
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SMILES
O=C1C2=C(CCN1CC)C=C(C3=NC(NC4=NC=C(N5CCNCC5)C=C4)=NC=C3F)C=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CDK4/6-IN-30 関連分類
HY-189130 関連分類
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