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CAS No. : 1619903-54-6
MCE 国际站:LY2857785
产品活性:LY2857785 是一种I型可逆的 ATP 竞争性的 CDK9,CDK8 和 CDK7 抑制剂,IC50 分别为 11 nM,16 nM 和 246 nM。
研究领域:Cell Cycle/DNA Damage | Apoptosis
作用靶点:CDK | Apoptosis
In Vitro: LY2857785 shows good selectivity against a panel of 114 protein kinases, with only 5 other protein kinases inhibited with potency (IC50) less than 0.1 μM, and a total of 14 kinases less than 1 μM. At the cellular level, LY2857785 inhibits CTD P-Ser2 and CTD P-Ser5 in U2OS cells at IC50s 0.089 (n=13) and 0.042 (n=1) μM, respectively. However, LY2857785 only induces a moderate G2-M DNA content increase, from 35% to 55%, with EC50 0.135 μM. LY2857785 shows potent compound exposure- and time-dependent cell proliferation inhibition in MV-4-11, RPMI8226, and L363 cells. When incubated between 4 to 24 hours, the cell growth inhibition potency reaches a maximal effect at 8 hours with IC50s 0.04, 0.2, and 0.5 μM for MV-4-11, RPMI8226, and L363 cells, respectively. LY2857785-induced cancer cell apoptosis is also time dependent, reaching maximal potency at 8 hours with IC50 0.5 μM in L363 cells.
In Vivo: In HCT116 xenograft tumor-bearing mice, LY2857785 demonstrates dose-dependent RNAP II CTD P-Ser2 inhibition potently with TED50 of 4.4 mg/kg and TEC50 of 0.36 μM. LY2857785 also shows significant duration of CTD P-Ser2 inhibition for 3 to 6 hours at TED70 (8 mg/kg) in HCT116 and MV-4-11 nude mice xenograft models. In the nude rat MV-4-11 xenograft model, LY2857785 similarly shows dose-dependent CTD P-Ser2 inhibition for 8 hours at TED70 (7 mg/kg) and TED90 (10 mg/kg). LY2857785 demonstrates the most dramatic tumor regression in the AML MV-4-11 xenograft tumor model either by i.v. bolus in mice or i.v. infusion in rats.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Covalent Screening Library | Anti-Breast Cancer Compound Library | Anti-Blood Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | SY-5609 | BRD4 Inhibitor-18 | 8α-Tigloyloxyhirsutinolide 13-O-acetate | CLK1/2-IN-1 | AAPK-25 | Dutasteride-13C6 | Oleic acid-13C | 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 | AT9283 | Staurosporine | SNS-032 | AZA1 | Antitumor agent-96
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货号: HY-12293
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