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Alisertib (MLN8237) - 10mM in DMSO, high purity , CAS No.1028486-01-2(DMSO), Serine/threonine-protein kinase Aurora-A inhibitor

COA COA
In stock
Item Number
A408546
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Availability
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A408546-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$277.90
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Aurora A Selective Inhibitors

View related series
Compound libraries (12325)

Basic Description

Synonyms Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Serine/threonine-protein kinase Aurora-A inhibitor
Product Description

Information

Alisertib (MLN8237) is a selectiveAurora Ainhibitor withIC50of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest,apoptosisandautophagy. Phase 3.
In vitro

MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone H3 phosphorylation. MLN8237 significantly inhibits cell proliferation in multiple myeloma (MM) cell lines with IC50 values of 0.003-1.71 μM. MLN8237 displays more potent anti-proliferation activity against primary MM cells and MM cell lines in the presence of BM stroma cells, as well as IL-6 and IGF-1 than against MM cells alone. MLN8237 (0.5 μM) induces 2- to 6-fold increase in G2/M phase in primary MM cells and cell lines, as well as significant apoptosis and senescence, involving the up-regulation of p53, p21 and p27, as well as PARP, caspase 3, and caspase 9 cleavage. In addition, MLN8237 shows strong synergistic anti-MM effect with dexamethasone, as well as additive effect with doxorubicin and bortezomib. MLN8237 (0.5 μM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with cisplatin (2.5 μM), involving the higher induction of TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment.

In vivo

MLN8237 significantly reduces the tumor burden with tumor growth inhibition (TGI) of 42% and 80% at 15 mg/kg and 30 mg/kg, respectively, and prolongs the survival of mice compared with the control.
Cell Data

cell lines：

Concentrations：Dissolved in DMSO, final concentrations ~10 μM

Incubation Time：24, 48, and 72 hours

Powder Purity:≥99%

Product Properties

ALogP 5.954
hba_count 6
HBD Count 1
Rotatable Bond 6

Associated Targets(Human)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
DNAJA1 Tchem DnaJ homolog subfamily A member 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MCM4 Tchem DNA replication licensing factor MCM4 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AURKA Tchem Aurora kinase A (15 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AURKB Tchem Aurora kinase B (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ACAD10 Tchem Acyl-CoA dehydrogenase family member 10 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
GNAI2 Tchem Guanine nucleotide-binding protein G(i) subunit alpha-2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles COC1=C(C(=CC=C1)F)C2=NCC3=C(N=C(NC4=CC(=C(C=C4)C(O)=O)OC)N=C3)C5=C2C=C(Cl)C=C5
Molecular Weight 518.92
Reaxy-Rn 18350078
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18350078&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 62 mg/mL warmed with 50ºC Water: bath (198.48 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility 27
DMSO(mM) Max Solubility 52.03
Water(mg / mL) Max Solubility <1

Solution Calculators

Reviews

Customer Reviews

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