1028486-06-7
1028486-06-7 structure
- Name: Alisertib sodium
- Chemical Name: sodium,4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoate
- CAS Number: 1028486-06-7
- Molecular Formula: C27H19ClFN4NaO4
- Molecular Weight: 540.90500
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-07-04 09:45:05
- Modify Date: 2025-08-21 12:50:07
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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[1][2][3].
| Name | sodium,4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoate |
|---|---|
| Synonyms |
UNII-23KN826MQ4
Alisertib sodium anhydrous |
| 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[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
Aurora A:12.5 nM (IC50) Aurora B:396.5 nM (IC50) |
| 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[1]. 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[2]. Alisertib (MLN 8237) inhibits cell proliferation with IC50s ranging from 15 to 469 nM in different tumer cell lines[4]. |
| 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[1]. Alisertib (3-30 mg/kg; P.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models[4]. Animal Model: Nude mice bearing HCT-116 colon tumor xenograft[4] Dosage: 3, 10, or 30 mg/kg Administration: P.o.; once daily for 3 weeks Result: Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively. |
| References |
| Molecular Formula | C27H19ClFN4NaO4 |
|---|---|
| Molecular Weight | 540.90500 |
| Exact Mass | 540.09800 |
| PSA | 108.76000 |
| LogP | 3.92000 |