- 貨號 Cat. No.
- S2898
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
MLN0905
Catalog No.S2898
MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.
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2mg |
USD 185 |
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5mg |
USD 239 |
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25mg |
USD 718 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. |
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Targets |
PLK1 |
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IC50 |
2 nM[1] |
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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] |
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Features |
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Protocol(Only for Reference)
Kinase Assay: [1]
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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Cell Assay: [1]
Cell lines |
HT-29 |
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Concentrations |
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Incubation Time |
72 h |
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Method |
Eight μL of serially diluted test compounds are added to75μL of HT29 (2.66 × 10 4 cells/well) cells in McCoy’s 5A media supplemented with 10% Fetal Calf Serum in Biocoat Poly-D lysine 384 well Black/Clear plates. Cells are incubated for 72 h at 37 ℃. Supernatant is aspirated from the wells, leaving 25μL in each well. ATP-lite 1 step reagent is added to each well, and luminescence for each plate is read on the LeadSeeker. Percent inhibition is calculated using the values from a DMSO control set to 100%. |
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Animal Study: [1]
Animal Models |
Nude mice bearing HT-29 xenografts |
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Dosages |
6.25 mg/Kg – 50 mg/Kg |
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Administration |
p.o. |
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1
References
Download MLN0905 SDF
Molecular Weight (MW) |
486.56 |
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Formula |
C24H25F3N6S
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CAS No. |
1228960-69-7 |
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Storage |
3 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
N/A |
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Solubility (25°C) * |
In vitro |
DMSO |
97 mg/mL (199 mM) |
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Water |
<1 mg/mL (<1 mM) |
Ethanol |
<1 mg/mL (<1 mM) |
* <1 mg/ml means slightly soluble or 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 Name |
6H-Pyrimido[5,4-d][1]benzazepine-6-thione, 2-[[5-[3-(dimethylamino)propyl]-2-methyl-3-pyridinyl]amino]-5,7-dihydro-9-(trifluoromethyl)- |
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Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
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Mass(mg) |
0.48656 |
4.8656 |
9.7312 |
14.5968 |
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