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CAS No. : 693228-63-6
MCE 国际站:CYC-116
产品活性:CYC-116是有效的极光激酶A和B (aurora A/B) 的抑制剂,Ki 值分别为8和9 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:Aurora Kinase
In Vitro: CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. CYC-116 shows potent antiproliferative activity against cancer cell lines with with IC50s of 0.599, 0.59, 0.241, 0.34, 0.725, 1.375, 0.471, 0.034, 0.372, 0.681, 0.151, 1.626, 0.775, 0.308, 0.110, 0.09 for MCF7, HeLa, Colo205, HCT-116, HT29, K562, CCRF-CEM, MV4-11, HL60, NCI-H460, A2780, BxPC3, HuPT4, Mia-Paca-2, Saos-2, Messa cells. Treatment with 1.25 μM CYC-116 for 7 h results in complete inhibition of histone H3 phosphorylation in HeLa cell lysates.
In Vivo: Oral administration of CYC-116 at dose levels of 75 and 100 mg/kg q.d. causes tumor growth delays of 2.3 and 5.8 days, which translates into specific growth delays of 0.32 and 0.81, respectively. The mean relative tumor volumes of mice receiving CYC-116 at both dose levels are less than those of vehicle-treated mice for the duration of the study period. At 100 mg/kg po q.d., the reduction in growth is statistically significant on days 6 and 9.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Anti-Blood Cancer Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | AAPK-25 | AT9283 | Aurora kinase inhibitor-3 | Aurora Kinases-IN-2 | ENMD-2076 Tartrate | Barasertib-HQPA | dAURK-4 | AMG 900 | SCH-1473759 | Aurora A inhibitor 1 | BI-847325 | CCT129202 | Tripolin A | ZM-447439 | LY3295668 | TAK-632 | Aurora inhibitor 1 | MK-8745 | Ilorasertib | JB170 | PHA-680632 | Aurora kinase inhibitor-8 | SNS-314 | Hesperadin | Tozasertib | Alisertib | Aurora A/PKC-IN-1 | Derrone | KW-2449
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货号: HY-10558
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