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CYC-116

CAS No. : 693228-63-6

MCE 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，K_i 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 K_is 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  |  AT9283  |  KW-2449  |  PF-03814735  |  ZM-447439  |  SNS-314 mesylate  |  CCT 137690  |  SCH-1473759 hydrochloride  |  NU6140  |  Aurora kinase inhibitor-2  |  Tripolin A  |  Aurora B inhibitor 1  |  Aurora inhibitor 1

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