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CAS No. : 741713-40-6
MCE 国际站:R547
产品活性:R547 是一种高效、选择性的,口服有效的 ATP 竞争性的 CDK 抑制剂,对 CDK1/cyclin B、 CDK2/cyclin E 和 CDK4/cyclin D1 作用的 Ki 值分别为 2 nM、3 nM、1 nM。
研究领域:Cell Cycle/DNA Damage | PI3K/Akt/mTOR | Stem Cell/Wnt | Apoptosis
作用靶点:CDK | GSK-3 | Apoptosis
In Vitro: R547 effectively inhibits CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1 (Ki = 1–3 nmol/L) and is inactive (Ki > 5,000 nmol/L) against a panel of >120 unrelated kinases in cell-free assays.
R547 effectively inhibits the proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50s <0.60 μM.
R547 reduces phosphorylation of the cellular retinoblastoma protein at specific CDK phosphorylation sites at the same concentrations that induced cell cycle arrest.
R547 has anti-proliferative activity in tumor cells independent of p53, retinoblastoma, or MDR status.
R547 blocks tumor cells in G1 plus G2 and induces apoptosis.
R547 induces apoptosis as measured by DNA fragmentation.
R547 inhibits phosphorylation of retinoblastoma protein in humantumor cells.
In Vivo: R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing.
R547 inhibits phosphorylation of retinoblastoma protein in tumors.
相关产品:Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Anti-Alzheimer's Disease Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Neurodegenerative Disease-related Compound Library | Anti-Obesity Compound Library | Glucose Metabolism Compound Library | Targeted Diversity Library | Antidepressant Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | SY-5609 | BRD4 Inhibitor-18 | 8α-Tigloyloxyhirsutinolide 13-O-acetate | CLK1/2-IN-1 | AAPK-25 | Dutasteride-13C6 | Oleic acid-13C | BRD5648 | Anticancer agent 120 | MFH290 | Abacavir sulfate | Meloxicam-d3-1 | Thailanstatin D | SB-218078 | Toyocamycin | Sorafenib-d4 | (S)-LY3177833 hydrate | Busulfan | PTC-028 | Dinaciclib | EGFR/HER2/CDK9-IN-2 | CR-1-31-B | CDK8-IN-11 | 142I5 | Farudodstat | Ecteinascidin 770 | AR-A014418 | AT9283 | Staurosporine | SNS-032
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货号: HY-10014
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