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PF-03814735

CAS No. : 942487-16-3

MCE 站：PF-03814735

产品活性：PF-03814735是有效，有口服性，ATP 竞争性的，可逆的极光激酶A和B (aurora A/B) 的抑制剂，IC₅₀值分别为0.8和5 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Protein Tyrosine Kinase/RTK

作用靶点：Aurora Kinase  |  VEGFR

In Vitro: In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. Small cell lung cancer (SCLC) and, to a lesser extent, colon cancer lines are very sensitive to PF-03814735. The status of the Myc gene family and retinoblastoma pathway members significantly correlates with the efficacy of PF-03814735.

In Vivo: Once-daily oral administration of PF-03814735 to mice bearing human xenograft tumors produces a reduction in phosphohistone H3 in tumors at doses that are tolerable and that result in significant inhibition of tumor growth. The combination of PF-03814735 and docetaxel in xenograft mouse tumor models shows additive tumor growth inhibition. PF-03814735 is much more effective in NCI-H82 xenografts when administered on a weekly dosing schedule at 80 mg/kg compared with a daily schedule at 15 mg/kg. PF-03814735 delayed growth by 23.5 days on the weekly schedule, which corresponds to 0.9 logs of net cell kill during the course of treatment.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Bevacizumab  |  Sunitinib  |  Semaxinib  |  SU 5402  |  PD173074  |  5Z-7-Oxozeaenol  |  Cediranib  |  SAR131675  |  AT9283  |  Gandotinib  |  KW-2449  |  GW806742X  |  Tanshinone IIA  |  ZM-447439  |  SNS-314 mesylate  |  Vatalanib dihydrochloride  |  CP-547632  |  AST 487  |  Tyrphostin A9  |  Ki20227  |  Motesanib  |  SU14813  |  Ramucirumab  |  SU1498  |  MAZ51  |  PP121  |  CCT 137690  |  Ki8751

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