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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Cell Cycle>Aurora Kinase Inhibitors>MLN-8237

MLN-8237

US $1.00 / 1KG

Min. Order: 1G
Purity: 98%
Cas No.: 1028486-01-2
Supply Ability: 100KG
  • 1KG

Overview

Product Name: MLN-8237
CAS No.: 1028486-01-2
EC-No.:
Min. Order: 1G
Purity: 98%
Supply Ability: 100KG
Release date: 2019/07/06
Product Advantage

AD68

MLN-8237 Basic information
Description In vitro In vivo
Product Name: MLN-8237
Synonyms: Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-;MLN-8237 4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid;alisertib (auroura A kinase inhibitor);Fluorocyclopentenylcytosine;4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth;MLN-823;4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid;MLN-8237
CAS: 1028486-01-2
MF: C27H20ClFN4O4
MW: 518.9235032
EINECS: 1592732-453-0
Product Categories: Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitor;API
Mol File: 1028486-01-2.mol
MLN-8237 Structure
 
MLN-8237 Chemical Properties
 
Safety Information
MSDS Information
 
 
MLN-8237 Usage And Synthesis
Description 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. 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. [1] 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.
Chemical Properties Off-White Solid
Uses An Aurora kinase inhibitor, used to treat patients with advanced solid tumors.
 

Country:China

Business model: Trader,Manufacturer

CB index: 58

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