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| | MLN0905 Basic information |
| Product Name: | MLN0905 | | Synonyms: | MLN0905;2-[[5-[3-(Dimethylamino)propyl]-2-methyl-3-pyridinyl]amino]-5,7-dihydro-9-(trifluoromethyl)- 6H-pyrimido[5,4-d][1]benzazepine-6-thione;6H-Pyrimido[5,4-d][1]benzazepine-6-thione, 2-[[5-[3-(dimethylamino)propyl]-2-methyl-3-pyridinyl]amino]-5,7-dihydro-9-(trifluoromethyl)-;2-[[5-[3-(Dimethylamino)propyl]-2-methyl-3-pyridinyl]amino]-5,7-dihydro-9-(trifluoromethyl)- 6H-pyrimido[5,4-d][1]benzazepine-6-thione MLN0905;MLN0905 2-[[5-[3-(Dimethylamino)propyl]-2-methyl-3-pyridinyl]amino]-5,7-dihydro-9-(trifluoromethyl)- 6H-pyrimido[5,4-d][1]benzazepine-6-thione;PLK1 Inhibitor;CS-1458;PLK1 INHIBITOR; MLN 0905; MLN-0905 | | CAS: | 1228960-69-7 | | MF: | C24H25F3N6S | | MW: | 486.56 | | EINECS: | | | Product Categories: | API;Inhibitors | | Mol File: | 1228960-69-7.mol |  |
| | MLN0905 Chemical Properties |
| Boiling point | 624.4±65.0 °C(Predicted) | | density | 1.37±0.1 g/cm3 (20 ºC 760 Torr) | | storage temp. | Store at -20°C | | solubility | ≥24.35 mg/mL in DMSO | | form | solid | | pka | 9.80±0.20(Predicted) |
| | MLN0905 Usage And Synthesis |
| Biological Activity | mln0905 is a potent inhibitor of plk1 with ic50 value ranges from 3 to 24 nm [1].polo-like kinase 1 (plk1) is a family of conserved serine/threonine kinases and plays an important role in regulating cell cycle. it has been revealed that plk1 drives cell cycle progression by triggerting g2/m transition and is considered as a pro-oncogene which overexpressed in tumor cells [2].mln0905 is a selective plk1 inhibitor and has similar effect as rnai hnockdown. when tested with ht-29 cells, mln0905 treatment significantly increased phish3 expression which indicated that cells were arrested in g2/m phase by inhibiting plk1 expression [1].in mouse model with human diffuse large b-cell lymphoma (dlbcl) cell line ocily-19 subcutaneous xenograft, co-administration of mln0905 and rituximab markedly reduced tumor volume and increased survival time through inhibiting plk1 which resulted in mitotic arrest [1]. and the same result was achieved when using nude mice model with human colon tumor ht29 xenograft, mln0905 treatment significantly inhibited tumor growth or progression [3]. | | target | PLK1 | | references | [1]. shi, j.q., et al., mln0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large b-cell lymphoma. mol cancer ther, 2012. 11(9): p. 2045-53.
[2]. espeut, j., et al., natural loss of mps1 kinase in nematodes uncovers a role for polo-like kinase 1 in spindle checkpoint initiation. cell rep, 2015.
[3]. duffey, m.o., et al., discovery of a potent and orally bioavailable benzolactam-derived inhibitor of polo-like kinase 1 (mln0905). j med chem, 2012. 55(1): p. 197-208. |
| | MLN0905 Preparation Products And Raw materials |
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