Alisertib 99%
Supplier: SELLECK CHEMICALS LLC MS
Synonyms:
4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido[4,5-e]azepin-2-yl)amino)-2-methoxybenzoic acid, MLN8237
Alisertib (MLN8237) is a selective aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay
- First orally available inhibitor of aurora A
- Powder
- 27 mg/mL (in DMSO)
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.
It has greater than 200-fold higher selectivity for aurora A than aurora B. phase 3.
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Formula:
C₂₇H₂₀ClFN₄O₄ MW: 518.92 g/mol Storage Temperature: Freezer |
MDL Number:
MFCD16621243 CAS Number: 1028486-01-2 |
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