MLN0905
- CAS NO.:1228960-69-7
- Empirical Formula: C24H25F3N6S
- Molecular Weight: 486.56
- MDL number: MFCD22683863
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:16
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) |
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
New Products
6-Bromo 2-Iodo Indole Pyridine 2,4,6-Tricarboxaldehyde Fosfomycin EP impurity D Ivermectin EP Impurity B Rimegepant Impurity 3 Tubulysin A Tubulysin B (R)-tert-butyl (4-methyl-1-oxopentan-3-yl)carbamate Tubulysin C Tubulysin E 2,2-diethoxyethanethioamide Calcium Sodium Phosphosilicate IH 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile Imeglimin Hydrochloride IH (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol 2-(3,5-Di-tert-butylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane Methyl 4-amino-3-(pyrrolidin-1-yl)benzoate 1-(4-Fluorophenyl)piperidin-2-one (1-Isopropyl-1H-pyrazol-5-yl)boronic acid 1-(4-Chlorophenyl)piperidin-2-one 3,6-Bis(4-iodophenyl)-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-dione 6-Bromo-2-methoxy-3-(4-methyl-1H-imidazol-1-yl)pyridineRelated products of tetrahydrofuran
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