MLN0905

Alias: PLK1 inhibitor; MLN0905; MLN 0905; MLN-0905
Cat No.:V1578 Purity: ≥98%
MLN0905 (MLN-0905; MLN 0905) is a novel, potent and selective small-molecule inhibitor of polo-like kinase-1 (PLK1) with potential antineoplastic activity.
MLN0905 Chemical Structure CAS No.: 1228960-69-7
Product category: PLK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

MLN0905 (MLN-0905; MLN 0905) is a novel, potent and selective small-molecule inhibitor of polo-like kinase-1 (PLK1) with potential antineoplastic activity. Its IC50 is 2 nM, which inhibits PLK1. A wide variety of human tumor cells, including DLBCL cell lines, are inhibited in their ability to proliferate by MLN0905. In several DLBCL models, pharmacodynamic pHisH3 modulation and strong antitumor activity are the results of PLK1 inhibition. These findings strongly support testing PLK1 inhibitors as DLBCL anticancer drugs in clinical settings.

Biological Activity I Assay Protocols (From Reference)
Targets
PLK1 (IC50 = 2 nM)
ln Vitro

MLN0905, having an IC50 of 2 nM, is a strong PLK1 inhibitor. MLN0905 has an EC50 of 9 nM, which inhibits cell mitosis. With an EC50 of 29 nM, MLN0905 directly readouts PLK1 inhibition by inhibiting Cdc25C-T96 phosphorylation. HT-29 viability is inhibited by MLN0905, with an LD50 of 22 nM. Reasonable selectivity against a panel of 359 kinases is exhibited by MLN0905.[1] With an IC50 of 3–24 nM, MLN0905 suppresses the viability of a panel of lymphoma cells.[2]

ln Vivo
After receiving MLN0905 (6.25 mg/Kg - 50 mg/Kg, p.o.) for 48 hours, naked mice with HT-29 xenografts exhibit dose-dependent pharmacodynamic responses. When MLN0905 (3.12 mg/Kg – 6.25 mg/Kg, p.o.) is given to OCI LY-19-Luc tumor-bearing mice, there are notable pharmacodynamic responses that peak eight hours after treatment.[1] When treated for 21 days with OCI LY-19-Luc xenografts containing scid mice, MLN0905 demonstrates antitumor efficacy. For the 6.25 mg/kg daily group, the T/C is 0.15.[2]
Enzyme Assay
Thirty microliters of human PLK1 enzymatic reaction were used, along with 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 0.02% BSA, 10% glycerol, 1 mM DTT, 100 mM NaCl, 3.3% DMSO, eight microliters of ATP, 0.2 microliters of [γ-33P]-ATP, four microliters of peptide substrate (Biotin-AHX-LDETGHLDSSGLQEVHLA-CONH2), and ten nanoliters of recombinant human PLK1[2–369]T210D. PLK inhibitors or not, the enzymatic reaction mixture is incubated for 2.5 hours at 30 degrees Celsius before being stopped with 20 microliters of 150 mM EDTA. After that, 25μL of the stopped enzyme reaction mixture is put on an Image FlashPlate coated with streptavidin that has 384 wells, and it is left to sit at room temperature for three hours. After three Tween-20 washes (0.02%), the Image Flash Plate wells are read using a Perkin-Elmer Viewlux.
Cell Assay
MLN0905 functions similarly to RNAi knockdown and is a selective PLK1 inhibitor. MLN0905 treatment dramatically increased pHisH3 expression in HT-29 cells, indicating that PLK1 expression was inhibited and cell arrest in the G2/M phase resulted.
Animal Protocol
Tumor (HT29) xenograft model
0-50 mg/kg
P.O; daily, QD×3/week
References

[1]. J Med Chem . 2012 Jan 12;55(1):197-208.

[2]. Mol Cancer Ther . 2012 Sep;11(9):2045-53.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H25F3N6S
Molecular Weight
486.56
Exact Mass
486.18
Elemental Analysis
C, 59.24; H, 5.18; F, 11.71; N, 17.27; S, 6.59
CAS #
1228960-69-7
Appearance
Solid powder
SMILES
CC1=C(C=C(C=N1)CCCN(C)C)NC2=NC=C3CC(=S)NC4=C(C3=N2)C=CC(=C4)C(F)(F)F
InChi Key
CODBZFJPKJDNDT-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H25F3N6S/c1-14-19(9-15(12-28-14)5-4-8-33(2)3)31-23-29-13-16-10-21(34)30-20-11-17(24(25,26)27)6-7-18(20)22(16)32-23/h6-7,9,11-13H,4-5,8,10H2,1-3H3,(H,30,34)(H,29,31,32)
Chemical Name
2-[[5-[3-(dimethylamino)propyl]-2-methylpyridin-3-yl]amino]-9-(trifluoromethyl)-5,7-dihydropyrimido[5,4-d][1]benzazepine-6-thione
Synonyms
PLK1 inhibitor; MLN0905; MLN 0905; MLN-0905
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~97 mg/mL (~199.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0552 mL 10.2762 mL 20.5524 mL
5 mM 0.4110 mL 2.0552 mL 4.1105 mL
10 mM 0.2055 mL 1.0276 mL 2.0552 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Biological Data
  • MLN0905

    MLN0905 induces a significant antitumor response in mice bearing disseminated (human) OCI LY-19-Luc lymphoma disease.

    MLN0905

    pHisH3 was used as a biomarker to determine the level of mitotic arrest in OCI LY-19-Luc xenograft tumors.2012 Sep;11(9):2045-53.

  • MLN0905

    MLN0905, a small-molecule inhibitor of PLK1, phenocopies the effects of PLK1 knockdown using RNAi in HT-29 cells.

    MLN0905

    MLN0905 induces a significant antitumor response in a primary human lymphoma model (PHTX-22L).2012 Sep;11(9):2045-53.

  • MLN0905

    MLN0905 and rituximab yield a synergistic antitumor response in a disseminated xenograft model of human lymphoma (OCI LY-19-Luc).

    MLN0905

    Evaluating the effect of dosing schedule versus antitumor effect with MLN0905 in the OCI LY-10 subcutaneous tumor model.2012 Sep;11(9):2045-53.

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