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Chemical Structure| 693228-63-6 Chemical Structure| 693228-63-6

Structure of CYC-116
CAS No.: 693228-63-6

Chemical Structure| 693228-63-6

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CYC116 is a potent inhibitor of Aurora with Ki of 8.0 nM/9.2 nM for Aurora A/B.

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Product Details of CYC-116

CAS No. :693228-63-6
Formula : C18H20N6OS
M.W : 368.46
SMILES Code : NC1=NC(C)=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)S1
MDL No. :MFCD14155805
InChI Key :GPSZYOIFQZPWEJ-UHFFFAOYSA-N
Pubchem ID :6420138

Safety of CYC-116

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CYC-116

epigenetics
DNA
RTK

Isoform Comparison

Biological Activity

Target
  • Aurora A

    Aurora A, Ki:8 nM

  • Aurora B

    Aurora B, Ki:9 nM

  • VEGFR2

    VEGFR2, Ki:44 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
COS7 cells 50 μM 24 h To screen and validate small molecules that can activate MISR2 signaling PMC9169708
HEK293T cells 10,000 nM 72 h Screened 525 anticancer agents and identified CYC-116 as showing greater toxicity in cells deficient in CYP2D6 activity PMC11490764
Dopaminergic neurons 0.5–3 µM Evaluate the inhibitory effect of CYC-116 on PINK1 kinase activity, results show that CYC-116 can inhibit PINK1 kinase activity. PMC10987619
HeLa cells 0.5–3 µM Evaluate the inhibitory effect of CYC-116 on PINK1 kinase activity, results show that CYC-116 can inhibit PINK1 kinase activity. PMC10987619
Bone marrow-derived mast cells (BMMCs) 0.2-15 µM 30 min CYC116 reversibly inhibited antigen-induced mast cell degranulation (IC50 ~1.42 µM) and secretion of TNF-α (IC50 ~1.10 µM) and IL-6 (IC50 ~1.24 µM) without cytotoxicity. PMC6513188

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Passive cutaneous anaphylaxis (PCA) and passive systemic anaphylaxis (PSA) models Oral 10, 30, 100 mg/kg Single dose, administered 1 h before antigen challenge in PCA CYC116 dose-dependently inhibited PCA (ED50 ~22.5 mg/kg) and PSA responses, with 100 mg/kg showing comparable efficacy to cetirizine (20 mg/kg). PMC6513188
Rats Neonatal rats Intraperitoneal injection 50 mg/kg Once daily for 10 days To evaluate the ability of CYC-116 to suppress ovarian folliculogenesis in vivo PMC9169708

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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