MLN82379 (Alisertib) 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.
J Hematol Oncol. 2017 Jun 8;10(1):115.
SIX3, a tumor suppressor, inhibits astrocytoma tumorigenesis by transcriptional repression of AURKA/B.
MLN8237 (Alisertib) purchased from AbMole
|Source||Journal of Hematology & Oncology (2017). Figure 7. MLN8237 (Abmole Bioscience)|
|Cell Lines||U251, U87 and U118 cell lines|
|Incubation Time||48 h|
|Results||Treatment with two other aurora kinase inhibitors, AZD1152 and MLN8237, demonstrated similar results (Fig. 7d).|
|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 (Roche).|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 26 mg/mL|
 Mosse YP et al. Clin Cancer Res. Pediatric Phase 1 Trial and Pharmacokinetic Study of MLN8237, an Investigational Oral Selective Small Molecule Inhibitor of Aurora Kinase A: A Children's Oncology Group Phase 1 Consortium study.
 Matulonis UA et al. Gynecol Oncol. Phase II study of MLN8237 (alisertib), an investigational Aurora A kinase inhibitor, in patients with platinum-resistant or -refractory epithelial ovarian, fallopian tube, or primary peritoneal carcinoma.
 Dees EC et al. Clin Cancer Res. Phase I Study of Aurora A Kinase Inhibitor MLN8237 in Advanced Solid Tumors: Safety, Pharmacokinetics, Pharmacodynamics, and Bioavailability of Two Oral Formulations.
 Cervantes A et al. Clin Cancer Res. Phase I Pharmacokinetic/Pharmacodynamic Study of MLN8237, an Investigational, Oral, Selective Aurora A Kinase Inhibitor, in Patients with Advanced Solid Tumors.
|Related Aurora Kinase Products|
LY3295668 (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
|Aurora Kinase Inhibitor III
Aurora Kinase Inhibitor III is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM.
SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively.
GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex.
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