Description
Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
Product information
CAS Number: 1028486-06-7
Molecular Weight: 540.91
Formula: C27H19ClFN4NaO4
Chemical Name: sodium 4-{[13-chloro-10-(2-fluoro-6-methoxyphenyl)-3,5,9-triazatricyclo[9.4.0.0²,⁷]pentadeca-1(15),2(7),3,5,9,11,13-heptaen-4-yl]amino}-2-methoxybenzoate
Smiles: [Na+].COC1=CC(=CC=C1C([O-])=O)NC1=NC2=C(CN=C(C3=C(F)C=CC=C3OC)C3=CC(Cl)=CC=C32)C=N1
InChiKey: AIUYVPGHBMKGAC-UHFFFAOYSA-M
InChi: InChI=1S/C27H20ClFN4O4.Na/c1-36-21-5-3-4-20(29)23(21)25-19-10-15(28)6-8-17(19)24-14(12-30-25)13-31-27(33-24)32-16-7-9-18(26(34)35)22(11-16)37-2;/h3-11,13H,12H2,1-2H3,(H,34,35)(H,31,32,33);/q;+1/p-1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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. The decreased activity of Alisertib (MLN 8237) for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A. Alisertib (MLN 8237) inhibits cell proliferation with IC50s ranging from 15 to 469 nM in different tumer cell lines.
In Vivo:
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.
Products are for research use only. Not for human use.
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