CYC116 - CAS 693228-63-6
Catalog number: 693228-63-6
Category: Inhibitor
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Aurora Kinase
CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
CYC116; CYC 116; CYC-116.
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Current Developer:
Cyclacel Pharmaceuticals, Inc
1.An integrated pharmacokinetic-pharmacodynamic model for an Aurora kinase inhibitor.
Kamei H1, Jackson RC, Zheleva D, Davidson FA. J Pharmacokinet Pharmacodyn. 2010 Aug;37(4):407-34. doi: 10.1007/s10928-010-9166-0. Epub 2010 Aug 8.
The spindle assembly checkpoint is a cell cycle surveillance mechanism that ensures the proper separation of chromosomes prior to cell division at mitosis. Aurora kinases play critical roles in mitotic progression and hence small-molecule inhibitors of Aurora kinases have been developed as a new class of potential anti-cancer drugs. In this paper we present for the first time an integrated pharmacokinetic-pharmacodynamic model of the functional effects of CYC116 (a known inhibitor of Aurora kinases A and B) on the spindle assembly checkpoint. We use the model to simulate two common experimental systems: cell culture and p.o. dosing of mice and present predictions of the effects of CYC116 for a range of doses and drug scheduling regimes. The model reveals that a critical peak drug concentration is required to cause aberrant kinetochore-microtubule attachments. The model also predicts that provided this threshold concentration is exceeded, a high total oral dose causes a high number of aberrant attachments within any given damaged cell.
2.Aurora kinase inhibitor patents and agents in clinical testing: an update (2011 - 2013).
Cheung CH1, Sarvagalla S, Lee JY, Huang YC, Coumar MS. Expert Opin Ther Pat. 2014 Sep;24(9):1021-38. doi: 10.1517/13543776.2014.931374. Epub 2014 Jun 26.
INTRODUCTION: Aurora kinase A, B and C, members of serine/threonine kinase family, are key regulators of mitosis. As Aurora kinases are overexpressed in many of the human cancers, small-molecule inhibitors of Aurora kinase have emerged as a possible treatment option for cancer.
3.Matrine and CYC116 synergistically inhibit growth and induce apoptosis in multiple myeloma cells.
Zhou YH1, Feng JY, You LS, Meng HT, Qian WB. Chin J Integr Med. 2015 Aug;21(8):635-9. doi: 10.1007/s11655-015-1975-y. Epub 2015 Mar 24.
OBJECTIVE: To investigate whether CYC116 can potentiate matrine-dependent growth inhibition and apoptosis in multiple myeloma (MM) cells.
4.Structural Biology Insight for the Design of Sub-type Selective Aurora Kinase Inhibitors.
Sarvagalla S, Coumar MS1. Curr Cancer Drug Targets. 2015;15(5):375-93.
Aurora kinase A, B and C, are key regulators of mitosis and are over expressed in many of the human cancers, making them an ideal drug target for cancer chemotherapy. Currently, over a dozen of Aurora kinase inhibitors are in various phases of clinical development. The majority of the inhibitors (VX-680/MK-0457, PHA-739358, CYC116, SNS-314, AMG 900, AT-9283, SCH- 1473759, ABT-348, PF-03814735, R-763/AS-703569, KW-2449 and TAK-901) are pan-selective (isoform non-selective) and few are Aurora A (MLN8054, MLN8237, VX-689/MK5108 and ENMD 2076) and Aurora B (AZD1152 and GSK1070916) sub-type selective. Despite the intensive research efforts in the past decade, no Aurora kinase inhibitor has reached the market. Recent evidence suggests that the sub-type selective Aurora kinase A inhibitor could possess advantages over pan-selective Aurora inhibitors, by avoiding Aurora B mediated neutropenia. However, sub-type selective Aurora kinase A inhibitor design is very challenging due to the similarity in the active site among the isoforms.
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CAS 693228-63-6 CYC116

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