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Formula | C18H20N6OS |
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Molecular Weight | 368.46 | CAS No. | 693228-63-6 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 24 mg/mL (65.13 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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. | |||||||||||
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Targets |
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In vitro | The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. [1] CYC116 is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that CYC116 has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. [1] In addition, anti-proliferative activity of CYC116 is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis. [1] | |||||||||||
In vivo | Mice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. [1] | |||||||||||
Features | An orally bioavailable, small molecule inhibitor of Aurora kinase/VEGFR2. |
Kinase Assay:[1] |
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Cell Assay: |
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Animal Study: |
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Data independently produced by Dr Zhang of Tianjin Medical University,
Inhibition of epigenetic and cell cycle-related targets in glioblastoma cell lines reveals that onametostat reduces proliferation and viability in both normoxic and hypoxic conditions [ Sci Rep, 2024, 14(1):4303] | PubMed: 38383756 |
DELs enable the development of BRET probes for target engagement studies in cells [ Cell Chem Biol, 2023, 30(8):987-998.e24] | PubMed: 37490918 |
A screen of repurposed drugs identifies AMHR2/MISR2 agonists as potential contraceptives [ Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119] | PubMed: 35380904 |
Inhibition of IκB Kinase Is a Potential Therapeutic Strategy to Circumvent Resistance to Epidermal Growth Factor Receptor Inhibition in Triple-Negative Breast Cancer Cells [ Cancers (Basel), 2022, 14(21)5215] | PubMed: 36358633 |
Using antagonistic pleiotropy to design a chemotherapy-induced evolutionary trap to target drug resistance in cancer. [ Nat Genet, 2020, 52(4):408-417] | PubMed: 32203462 |
Chemosensitivity and chemoresistance in endometriosis - differences for ectopic versus eutopic cells. [ Reprod Biomed Online, 2019, 10.1016/j.rbmo.2019.05.019] | PubMed: 31377021 |
An Anti-Cancer Drug Candidate CYC116 Suppresses Type I Hypersensitive Immune Responses through the Inhibition of Fyn Kinase in Mast Cells [ Biomol Ther (Seoul), 2019, 27(3):311-317] | PubMed: 30332888 |
Targeted Polo-like Kinase Inhibition Combined With Aurora Kinase Inhibition in Pediatric Acute Leukemia Cells. [ J Pediatr Hematol Oncol, 2019, 41(6):e359-e370] | PubMed: 30702467 |
Aurora Kinases as Druggable Targets in Pediatric Leukemia: Heterogeneity in Target Modulation Activities and Cytotoxicity by Diverse Novel Therapeutic Agents [Jayanthan A, et al. PLoS One, 2014, 9(7):e102741] | PubMed: 25048812 |
Targeting Sonic Hedgehog-Associated Medulloblastoma through Inhibition of Aurora and Polo-like Kinases. [Markant SL, et al. Cancer Res, 2013, 73(20):6310-22] | PubMed: 24067506 |
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