2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase HDAC Apoptosis
  4. Aurora kinase/HDAC-IN-1

Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model.

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Aurora kinase/HDAC-IN-1

Aurora kinase/HDAC-IN-1 Chemical Structure

CAS No. : 2727102-12-5

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Aurora kinase/HDAC-IN-1 Related Antibodies

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Aurora Kinase Aurora A Aurora B Aurora C

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model[1].

IC50 & Target[1]

Aurora A

116 nM (IC50)

Aurora B

225 nM (IC50)

HDAC1

164 nM (IC50)

HDAC2

346 nM (IC50)

In Vitro

Aurora kinase/HDAC-IN-1 (compound 6) (0.64 nM–10 μM; 72 h) inhibits HCT-116 and MIA PaCa-2 cell proliferation with IC50values of 30.2 nM and 42.8 nM, respectively[1].
Aurora kinase/HDAC-IN-1 (30-120 nM; 24 h) induces G2/M arrest in HCT-116 cells[1].
Aurora kinase/HDAC-IN-1 (30-120 nM; 48 h) induces apoptosis in HCT-116 cells[1].
Aurora kinase/HDAC-IN-1 (30-120 nM; 72 h) modulates Aurora/HDAC-related signaling in HCT-116 cells, including increased Ac-H3 and reduced Aurora A phosphorylation[1].

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

Aurora kinase/HDAC-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT-116 cells; MIA PaCa-2 cells
Concentration: 0.64 nM-10 μM
Incubation Time: 72 h
Result: Inhibited HCT-116 cell proliferation with an IC50 value of 30.2 nM.
Inhibited MIA PaCa-2 cell proliferation with an IC50 value of 42.8 nM.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 30 nM, 60 nM, 120 nM
Incubation Time: 24 h
Result: Increased G2/M-phase population from 5.03% (control) to 12.68% (30 nM), 20.17% (60 nM), and 25.40% (120 nM).

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 30 nM, 60 nM, 120 nM
Incubation Time: 48 h
Result: Increased apoptosis rate from 1.99% (control) to 21.03% (30 nM), 42.81% (60 nM), and 59.13% (120 nM).

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 30 nM, 60 nM, 120 nM
Incubation Time: 72 h
Result: Increased Ac-H3 expression and upregulated p53 and Caspase 3 expression, and reduced p-Aurora A levels.
Parmacokinetics
Species Dose Route CL Vdss AUC0-t T1/2 Cmax Tmax F
Mice 1 mg/kg i.v. 98.6 mL/min/kg 1.49 L/kg 168 ng·h/mL 0.307 h / / /
Mice 50 mg/kg p.o. / / 1850 ng·h/mL 5.73 h 448 ng/mL 1.00 h 23.2 %
In Vivo

Aurora kinase/HDAC-IN-1 (compound 6) (50-150 mg/kg/d; p.o.; QD; for 21 days) significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model (TGI = 71.8% at 150 mg/kg/d) and shows satisfactory oral bioavailability in mice (F = 23.2%)[1].

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

Animal Model: Female BALB/c nude mice (6-8 weeks old) bearing subcutaneous HCT-116 xenografts [1]
Dosage: 50 mg/kg/d, 150 mg/kg/d
Administration: Oral gavage (p.o.), once daily (QD), for 21 days.
Result: Inhibited tumor growth in HCT-116 colorectal cancer xenograft mice, resulting in a significant reduction in tumor volume without obvious toxicity.
Increased tumor necrosis and reduced Ki67 staining (decreased proliferation), with more pronounced effects at 150 mg/kg/d.
Molecular Weight

449.50

Formula

C22H20FN7OS
CAS No.
SMILES

O=C(C1=CC=C(CSC2=NC=CC(NC3=NNC(C)=C3)=N2)C=C1)NC4=CC=C(C=C4N)F
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Aurora kinase/HDAC-IN-1 Related Classifications

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  • 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.

Keywords:

Aurora kinase/HDAC-IN-12727102-12-5Aurora KinaseHDACApoptosisHistone deacetylasesAurora AAurora B,HDACdual inhibitorcolorectal cancerHCT-116 cellsxenograft modelInhibitorinhibitorinhibit

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