MLN0905
Catalog No.S2898
Molecular Weight(MW): 486.56
MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.
Cited by 2 publications
Purity & Quality Control
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Biological Activity
| Description | MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. | ||
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| In vitro |
MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. MLN0905 inhibits cell mitosis with EC50 of 9 nM. MLN0905 inhibits Cdc25C-T96 phosphorylation, a direct readout of PLK1 inhibition with EC50 of 29 nM. MLN0905 inhibits HT-29 viability with LD50 of 22 nM. MLN0905 possesses reasonable selectivity against a panel of 359 kinases. [1] MLN0905 inhibits a panel of lymphoma cells viability with IC50 of 3 – 24 nM. [2] |
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| In vivo | Nude mice bearing HT-29 xenografts administered with MLN0905 (6.25 mg/Kg - 50 mg/Kg, p.o.) shows dose-dependent pharmacodynamic responses (48 hours after treatment). OCI LY-19-Luc tumor bearing mice administered with MLN0905 (3.12 mg/Kg – 6.25 mg/Kg, p.o.) shows significant pharmacodynamic responses amd peaks at 8 hours after treatment. [1] MLN0905 shows antitumor efficacy in treatment with OCI LY-19-Luc xenografts bearing scid mice for 21 days. The T/C of 6.25 mg/Kg daily group is 0.15. [2] |
Protocol
| Kinase Assay:[1] |
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PLK1 Flash Plate Assay: The human PLK1 enzymatic reaction totaling 30μL contained 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 0.02% BSA, 10% glycerol, 1 mM DTT, 100 mM NaCl, 3.3% DMSO, 8 μM ATP, 0.2μCi [γ- 33 P]-ATP, 4μM peptide substrate (Biotin-AHX-LDETGHLDSSGLQEVHLA-CONH2), and 10 nM recombinant human PLK1[2–369]T210D. The enzymatic reaction mixture, with or without PLK inhibitors, is incubated for 2.5 h at 30℃before termination with 20μL of 150 mM EDTA. Then 25μL of the stopped enzyme reaction mixture is transferred to a 384-well streptavidin coated Image FlashPlate and incubated at room temperature for 3 h. The Image Flash Plate wells are washed three times with 0.02% Tween-20 and then read on the Perkin-Elmer Viewlux. |
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Solubility (25°C)
| In vitro | DMSO | 97 mg/mL (199.35 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 486.56 |
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| Formula | C24H25F3N6S |
| CAS No. | 1228960-69-7 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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