4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth
4-{[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoic acid
CAS: 1028486-01-2
Molecular Formula: C27H20ClFN4O4
4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth - Names and Identifiers
| Name | 4-{[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoic acid |
| Synonyms | MLN-823 MLN 8237 MLN8237 MLN-8237 ALISERTIB (MLN8237) Fluorocyclopentenylcytosine alisertib (auroura A kinase inhibitor) 4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth 4-{[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoic acid 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 |
| CAS | 1028486-01-2 |
| EINECS | 1592732-453-0 |
| InChI | InChI=1S/C27H20ClFN4O4/c1-36-21-5-3-4-20(29)23(21)25-19-10-15(28)6-8-17(19)24-14(12-30-25)13-31-27(33-24)32-16-7-9-18(26(34)35)22(11-16)37-2/h3-11,13H,12H2,1-2H3,(H,34,35)(H,31,32,33) |
4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth - Physico-chemical Properties
| Molecular Formula | C27H20ClFN4O4 |
| Molar Mass | 518.92 |
| Density | 1.43±0.1 g/cm3(Predicted) |
| Boling Point | 729.1±70.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 5 mg/ml) |
| Appearance | solid |
| Color | Off-white |
| pKa | 4.07±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | MLN8237 was more than 200-fold more selective for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM and no significant activity against 205 other kinases. Treatment of mm1. S and OPM1 cells with 0.5 μm MLN8237 inhibited Aurora A phosphorylation without affecting Aurora B- regulated histone H3 phosphorylation. MLN8237 significantly inhibited the proliferation of multiple myeloma (MM) cells with an IC50 of 0.003-1.71 μm. In the presence of BM stromal cells, IL-6 and IGF-1, MLN8237 acts on primary MM cells and MM cell lines with much higher antiproliferative activity than when only MLN8237 acts alone. 0.5 μm MLN8237 acts on primary MM cells and cell lines to increase G2/M phase cells by 2 to 6 times, and significantly induces apoptosis and senescence, involving the up-regulation of p53, p21 and p27, and cleavage of PARP,caspase 3, and caspase 9. In addition, the combination of MLN8237 and Dexamethasone has a synergistic effect with strong anti-MM efficacy, while the combination with Doxorubicin and Bortezomib has additional functions. Treatment of FLO-1, OE19, and OE33 esophageal adenocarcinoma cell lines with 0.5 μm MLN8237 inhibited colony formation and significantly increased the percentage of polyploid cells and subsequently the percentage of G1 phase cells, and with Cisplatin (2.5 μm), the effect is further improved, compared with the single drug, induced to produce more, TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP. MLN8237 was more than 200-fold more selective for Aurora A than structure-related Aurora B, with an IC50 of 396.5 nM, but was not significantly active against 205 other kinases. Treatment of mm1. S and OPM1 cells with 0.5 μm MLN8237 inhibited Aurora A phosphorylation without affecting Aurora B- regulated histone H3 phosphorylation. MLN8237 significantly inhibited the proliferation of multiple myeloma (MM) cells with an IC50 of 0.003-1.71 μm. In the presence of BM stromal cells, IL-6 and IGF-1, MLN8237 acts on primary MM cells and MM cell lines with much higher antiproliferative activity than when only MLN8237 acts alone. 0.5 μm MLN8237 acts on primary MM cells and cell lines to increase G2/M phase cells by 2 to 6 times, and significantly induces apoptosis and senescence, involving the up-regulation of p53, p21 and p27, and cleavage of PARP,caspase 3, and caspase 9. In addition, the combination of MLN8237 and Dexamethasone has a synergistic effect with strong anti-MM efficacy, while the combination with Doxorubicin and Bortezomib has additional functions. Treatment of FLO-1, OE19, and OE33 esophageal adenocarcinoma cell lines with 0.5 μm MLN8237 inhibited colony formation and significantly increased the percentage of polyploid cells, followed by the percentage of G1 phase cells, whereas with cisin (2.5 μm) the effect was further improved, and more TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP were induced compared with the single drug. |
| In vivo study | MLN8237 oral treatment, significantly reduced the tumor burden, 15 mg/kg and 30 mg/kg dose treatment of tumor growth inhibition (TGI) were 42% and 80%, and compared with the control group, delay the life span of mice. MLN8237 (30 mg/kg) combined with Cisplatin (2 mg/kg) on FLO-1 transplanted tumor, compared with the single drug, the anticancer activity was enhanced, accompanied by the inhibition of Ki-67 expression, nuclear p73 protein and cleaved caspase 3 expression were enhanced. oral administration of MLN8237 significantly reduced the tumor burden, with tumor growth inhibition rates (TGI) of 42% and 80% at doses of 15 mg/kg and 30 mg/kg, respectively, and compared with the control group, the life span of mice was delayed. MLN8237 (30 mg/kg) combined with Cisplatin (2 mg/kg) on FLO-1 transplanted tumor, compared with the single drug, the anticancer activity was enhanced, accompanied by the inhibition of Ki-67 expression, nuclear p73 protein and cleaved caspase 3 expression were enhanced. |
4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.927 ml | 9.635 ml | 19.27 ml |
| 5 mM | 0.385 ml | 1.927 ml | 3.854 ml |
| 10 mM | 0.193 ml | 0.964 ml | 1.927 ml |
| 5 mM | 0.039 ml | 0.193 ml | 0.385 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: Alisertib (MLN8237) Visit Supplier Webpage Request for quotationCAS: 1028486-01-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth
利克飞龙(纯度有争议)
利克飞龙(纯度有争议)