MLN8237 (Alisertib)

Cat. No. M1752

Synonym:

Alisertib

Size	Price	Availability
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 & Documentation

Purity: 99.17%
COA
MSDS
H-NMR
HPLC

Product Information

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

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

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 (for reference only)

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

Chemical Information

Molecular Weight	518.92
Formula	C27H20ClFN4O4
CAS Number	1028486-01-2
Solubility (25°C)	DMSO 26 mg/mL
Storage	Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month

Conversion of different model animals based on BSA (PMID: 27057123)

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
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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.

Related Aurora Kinase Products
Aurora Kinases-IN-4 Aurora Kinases-IN-4 is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM).
Derrone Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity.
CD532 hydrochloride CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer.
Aurora kinase inhibitor-2 Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.
AAPK-25 AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.

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