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Alisertib (MLN8237) is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. MLN8237 (Alisertib) binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. Alisertib (MLN 8237) leads the MM cells to mitotic spindle abnormalities, mitotic accumulation, as well as inhibition of cell proliferation through apoptosis and senescence. Alisertib up-regulates p53 and tumor suppressor genes p21 and p27.
Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM. Alisertib (3-30 mg/kg; p.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models.
J Hematol Oncol. 2017 Jun 8;10(1):115.
SIX3, a tumor suppressor, inhibits astrocytoma tumorigenesis by transcriptional repression of AURKA/B.
Alisertib purchased from AbMole
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Source | Journal of Hematology & Oncology (2017). Figure 7. MLN8237 (Abmole Bioscience) |
| Method | CCK8 assay | |
| Cell Lines | U251, U87 and U118 cell lines | |
| Concentrations | ||
| Incubation Time | 48 h | |
| Results | Treatment with two other aurora kinase inhibitors, AZD1152 and MLN8237, demonstrated similar results (Fig. 7d). |
| Cell Experiment | |
|---|---|
| Cell lines | HCT-116, SW480, DLD-1, H460, MDA-MB-231, PC3, SKOV3 cell lines |
| Preparation method | BrdU in vitro cell proliferation assay Thirteen tumor cell lines treated with increasing concentrations of alisertib over 96 hours were subjected to 5-bromo-2-deoxyuridine (BrdU) incorporation as a measurement of cellular proliferation. Proliferation of each cell line was measured using the cell proliferation ELISA, BrdU colorimetric kit according to the manufacturer's recommendations. |
| Concentrations | 0~1µM |
| Incubation time | 96h |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing the disseminated, CD20-positive, non-Hodgkin's lymphoma model OCI-LY19 |
| Formulation | 10% 2-hydroxypropyl-β-cyclodextrin and 1% sodium bicarbonate |
| Dosages | 20 mg/kg twice daily or 30 mg/kg once daily |
| Administration | oral gavage |
| Molecular Weight | 518.92 |
| Formula | C27H20ClFN4O4 |
| CAS Number | 1028486-01-2 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Aurora Kinase Products |
|---|
| AT9283
AT9283 is a potent inhibitor of several protein kinases, including Aurora A, Aurora B, Janus kinase 2 (JAK2), JAK3, and ABL. |
| AZD1152-HQPA
AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora with Ki values of 0.36 and 1369 nM for Aurora B and Aurora A respectively. |
| CCT-129202
CCT129202 is an Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively. |
| CYC116
CYC116 is a potent, small molecule inhibitor of Aurora A, B and C with IC50 value of 44, 19 and 65 nM respectively. 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. |
| ENMD-2076
ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor. |
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