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MLN8237 (Alisertib)

Cat. No. M1752
MLN8237 (Alisertib) Structure
Synonym:

Alisertib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 34  USD34 In stock
5mg USD 60  USD60 In stock
10mg USD 98  USD98 In stock
50mg USD 280  USD280 In stock
100mg USD 450  USD450 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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).
Protocol
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 (Roche).
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 518.92
Formula C27H20ClFN4O4
CAS Number 1028486-01-2
Purity 99.17%
Solubility DMSO 26 mg/mL
Storage at -20°C
References

[1] 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.

[2] 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.

[3] 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.

[4] 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.

[5] Muscal JA et al. Invest New Drugs. Additive effects of vorinostat and MLN8237 in pediatric leukemia, medulloblastoma, and neuroblastoma cell lines.

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  Catalog
Abmole Inhibitor Catalog




Keywords: MLN8237 (Alisertib), Alisertib supplier, Aurora Kinase, inhibitors

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