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

CYC-116 

Cat. No.: HY-10558 Purity: 98.17%
COA 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 92 In-stock
50 mg USD 343 In-stock
100 mg USD 640 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

CYC-116 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

CYC-116 Related Antibodies
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].

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

368.46

Appearance

Solid

Formula

C18H20N6OS
CAS No.
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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 15 mg/mL (40.71 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7140 mL 13.5700 mL 27.1400 mL
5 mM 0.5428 mL 2.7140 mL 5.4280 mL
10 mM 0.2714 mL 1.3570 mL 2.7140 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.5 mg/mL (4.07 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.5 mg/mL (4.07 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.17%

COA (246 KB) HNMR (165 KB) LCMS (377 KB)

Handling Instructions (2659 KB)
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
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CYC-116 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

CYC-116693228-63-6CYC116CYC 116Aurora KinaseInhibitorinhibitorinhibit

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