1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. CYC-116

CYC-116 

Cat. No.: HY-10558 Purity: 98.17%
Handling Instructions

CYC-116 is a potent aurora A and aurora B inhibitor with Kis of 8 and 9 nM, respectively.

For research use only. We do not sell to patients.

CYC-116 Chemical Structure

CYC-116 Chemical Structure

CAS No. : 693228-63-6

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10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 312 In-stock
Estimated Time of Arrival: December 31
100 mg USD 582 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

CYC-116 is a potent aurora A and aurora B inhibitor with Kis of 8 and 9 nM, respectively.

IC50 & Target[1]

Aurora A

8 nM (Ki)

Aurora B

9.2 nM (Ki)

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[1].

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[1].

Clinical Trial
Molecular Weight

368.46

Formula

C₁₈H₂₀N₆OS

CAS No.

693228-63-6

SMILES

CC1=C(SC(N)=N1)C2=NC(NC3=CC=C(C=C3)N4CCOCC4)=NC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)

H2O : < 0.1 mg/mL (insoluble)

References
Kinase Assay
[1]

Aurora A kinase assays are performed using a 25 μL reaction volume (25 mM β-glycerophosphate, 20 mM Tris/HCl, pH 7.5, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO4, 10 μg of kemptide (peptide substrate)), and recombinant aurora A kinase is diluted in 20 mM Tris/HCl, pH 8, containing 0.5 mg/mL BSA, 2.5% glycerol, and 0.006% Brij-35. Reactions are started by the addition of 5 μL Mg/ATP mix (15 mM MgCl4, 100 μM ATP, with 18.5 kBq γ-32P-ATP per well) and incubated at 30°C for 30 min before terminating by the addition of 25 μL of 75 mM H3PO4. Aurora B kinase assays are performed as for aurora A except that prior to use, aurora B is activated in a separate reaction at 30°C for 60 min with inner centromeres protein[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay

CYC-116 is prepared in DMSO and diluted in cell medium[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Mice implanted intraperitoneally with P388/0 cells are treated with CYC-116, and the antitumor activity is measured as an increase in lifespan of the treated animals versus the vehicle control group[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.17%

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Keywords:

CYC-116CYC116CYC 116Aurora KinaseInhibitorinhibitorinhibit

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CYC-116
Cat. No.:
HY-10558
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