ChemicalBook > CAS DataBase List > MLN0905
MLN0905
MLN0905
- CAS No.1228960-69-7
- Chemical Name:MLN0905
- CBNumber:CB72628151
- Molecular Formula:C24H25F3N6S
- Formula Weight:486.56
- MOL File:1228960-69-7.mol
MLN0905 Property
- 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
- pka 9.80±0.20(Predicted)
- form solid
- color Off-white to yellow
Safety
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H315-H319-H335
- Precautionary statements P261-P305+P351+P338
MLN0905 Chemical Properties,Usage,Production
- Uses MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer[1][2].
- 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].
-
in vivo
MLN0905 (p.o.; 50 mg/kg) shows a high sustained PD response in nude mice HT29 xenograft tumors[1].
MLN0905 (p.o.; 6.25, 12.5, 25, 50 mg/kg) exhibits significant antitumor activities in mice HT29 xenograft tumors[1].
MLN0905 (p.o.; 0-14.5 mg/kg; daily, QD×3/week) has marked antitumor effects in kinds of lymphoma xenograft model[1][2].Animal Model: Tumor (HT29) xenograft model[1] Dosage: 0-50 mg/kg Administration: P.O; daily, QD×3/week Result: Observed antitumor activity, tumor stasis or regression and well-tolerated oral doses. - target PLK1
- IC 50 PLK1: 2 nM (IC50)
-
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
Raw materials
Preparation Products
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1228960-69-7, MLN0905Related Search:
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- API
- Inhibitors
- 生物试剂
- 抑制剂
- 合成有机化合物配体
- 细胞生物学试剂
- 小分子抑制剂
- 小分子抑制剂,天然产物
- 细胞周期
- C24H25F3N6S
- 化合物MLN0905,10 MM DMSO 溶液
- 2-((5-(3-(二甲基氨基)丙基)-2-甲基吡啶-3-基)氨基)-9-(三氟甲基)-5,7-二氢-6H-苯并[B]嘧啶并[4,5-D]氮杂卓-6-硫酮
- PLK1抑制剂(MLN0905)
- 2-[[5-[3-(二甲基氨基)丙基]-2-甲基-3-吡啶基]氨基]-5,7-二氢-9-(三氟甲基)- 6H-嘧啶并[5,4-D][1]苯并氮杂卓-6-硫酮
- 1228960-69-7
- MLN0905, 10 mM in DMSO
- 2-((5-(3-(Dimethylamino)propyl)-2-methylpyridin-3-yl)amino)-9-(trifluoromethyl)-5,7-dihydro-6H-benzo[b]pyrimido[4,5-d]azepine-6-thione
- AI3-14412
- AI314412
- AI3 14412
- MLN0905 USP/EP/BP
- PLK1 INHIBITOR; MLN 0905; MLN-0905
- CS-1458
- PLK1 Inhibitor
- 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
- 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
- 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