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HomeProduct name listMLN0905

MLN0905

MLN0905 Structural

What is MLN0905?

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].

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.

Properties of MLN0905

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)
color  Off-white to yellow

Safety information for MLN0905

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for MLN0905

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