MLN-8237
| Price | $1 |
| Package | 1KG |
| Min. Order: | 1G |
| Supply Ability: | 100KG |
| Update Time: | 2019-07-06 |
Product Details
| Product Name: MLN-8237 | CAS No.: 1028486-01-2 |
| Min. Order: 1G | Purity: 98% |
| Supply Ability: 100KG | Release date: 2019/07/06 |
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 |
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| 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. |
Company Profile Introduction
Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals.
Mainly deals in the sales of:
Pharmaceutical intermediates
OLED intermediates：
Pharmaceutical intermediates;
OLED intermediates;
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China- Since: 2014-12-17
- Address: Zhengzhou High tech Zone, Henan Province, China
INQUIRY
楊俊青
sales@coreychem.com
sales@coreychem.com