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Aurora A Inhibitor I Chemical Structure
VX-680 (MK-0457, Tozasertib)
VX-680 (MK-0457, Tozasertib) is the inhibitor of Aurora-A,-B,-C kinases with apparent inhibition constant values of 0.6,18,4.6 nM respectively.
MLN8054
MLN8054 is an Aurora inhibitor, Aurora A (IC50 = 0.004 uM) over Aurora B (IC50 = 0.172 uM).
ZM-447439
ZM-447439 is a poten, selective ATP-competitive Aurora B kinase inhibitor with an IC50 of 50 nM, 1 μM and 250 nM for Aurora B, A and C, respectively.
Danusertib (PHA-739358)
Danusertib (PHA-739358) is a pyrrolo-pyrazole and small molecule aurora kinases and Bcr-Abl kinase inhibitor for aurora A, B, and C with IC50 of 13 nM, 79 nM, and 61 nM, respectively.
MLN8237 (Alisertib)
MLN8237 (Alisertib) is a selective Aurora kinase A inhibitor with a median IC50 of 61 nM.
AT9283
AT9283 is a small molecule a multi-targeted c-ABL, JAK2, Aurora A and B inhibitor with IC50 of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively.
AZD1152-HQPA (Barasertib)
AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora B (Ki, 0.36 nM)
SNS-314
SNS-314 Mesylate is a potent and selective Aurora kinase inhibitor with IC50 of 9, 31, and 3.4 nM for Aurora kinases A, B, and C, respectively.
CYC116
CYC116 is an Aurora kinase/VEGFR2 inhibitor
ENMD-2076
ENMD-2076 is a antiangiogenic and Aurora kinase inhibitor with IC50 of 3, 13, 350, 23, 40, 93 and 120 nM for Flt-3, AurA, AurB, Src, KDR/VEGFR2 and FGFR1.
Biological Activity
| Information | Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A with IC50 of 3.4 nM. | |||||
|---|---|---|---|---|---|---|
| Targets | Aurora A | Aurora B | Aurora C | |||
| IC50 | 3.4 nM | 3.4 μM [1] | 0.432 μM [2] | |||
| In vitro | Aurora A Inhibitor I is a 2,4-dianilinopyrimidine that selectively and potently inhibits Aurora A. Aurora A Inhibitor I effectively inhibits the proliferation of HCT116 and HT29 cells, with IC50 of 190 nM and 2.9 μM, respectively. The Aurora A selectivity of Aurora A Inhibitor I against Aurora B depends on a single amino acid (Thr217) of Aurora A. [1] In KCL-22 cells, Aurora A Inhibitor I (1–5 μM) increases G2/M cell fraction, induces histone H3 serine 10 phosphorylation, and suppresses mitotic Aurora A autophosphorylation on Thr288. Aurora A Inhibitor I (0.5–5 μM) also suppresses cell proliferation in KCL-22 cells, as well as BCR-ABL-negative leukemia cell lines KG-1 and HL-60. Aurora A Inhibitor I effectively induces apoptosis in KCL-22 cells at 5 μM. [2] In a recent study, Aurora A Inhibitor I is also found to inhibit cell growth of HCT116, HT29, and HeLa cells, with IC50 of 377.6 nM, 5.6 μM, and 416 nM. [3] | |||||
| In vivo | ||||||
| Clinical Trials | ||||||
| Features | Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A. | |||||
Protocol
Kinase Assay: [1]
| Auroras A and B Inhibition Assays | Both Auroras A and B are assayed in ELISA format using a GST fusion (pGEX-4T) of the N-terminus of Histone H3 (aa 1−18) as substrate. Plates are coated with 2 μg/mL substrate in PBS then blocked with 1 mg/mL I-block in PBS. Kinase reactions are run for 40 min with 5 ng/mL (0.16 nM) Aurora A or 45 ng/mL (1.1 nM) Aurora B at 30 μM ATP (~ Km) in kinase buffer. Final DMSO concentration is 4%. Product is detected by incubation with antiphosphohistone H3 (Ser10) 6G3 mouse monoclonal antibody and sheep-anti-mouse HRP conjugate, followed by washing and addition of TMB substrate. After quenching with 1 M phosphoric acid, plates are read at 450 nM. |
|---|
Cell Assay: [1]
| Cell lines: | HCT116 and HT29 cells |
|---|---|
| Concentrations: | 0.1 nM–10 μM, dissolved in medium lacking serum and glutamine (dissolved in DMSO as stock solution) |
| Incubation Time: | 72 hours |
| Method: | Cells are seeded in 384-well plates on day 0 in 50 μL of complete medium and incubated overnight in a 5% CO2 atmosphere at 37 ℃. On day 1, 10 μL of Aurora A Inhibitor I is added. On day 4, plates are allowed to reach room temperature, and 30 μL Cell Titer-Glo reagent is added to each well to measure total ATP levels. Plates are read after shaking 15 min at room temperature. |
Product Information
| Molecular Weight (WM): | 588.07 |
|---|---|
| Formula: | C31H31ClFN7O2 |
| CAS No.: | 1158838-45-9 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥118mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Western blot analysis of Histone and p-Histone. 0-10μM Aurora inhibitor I was added.
Western blot analysis of Histone and p-Histone. 0-10μM Aurora inhibitor I was added.
Data independently produced by Dr. Zhang of Tianjin Medical University Aurora A Inhibitor I purchased from Selleck
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Western blot analysis of Histone and p-Histone. 0-10μM Aurora inhibitor I was added.
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Data independently produced by Dr. Zhang of Tianjin Medical University
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