MLN0905

SKU: orb1305140

Description

MLN0905 is a potent and selective small molecule inhibitor of PLK1 with an IC50 of 2 nM. It is a valuable research tool for studying mitosis and cell cycle progression in vitro and has demonstrated antitumor activity in preclinical in vivo cancer models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1228960-69-7
• MW: 486.56
• Purity: 99.92% (May vary between batches)
• Formula: C₂₄H₂₅F₃N₆S
• SMILES: CN(C)CCCc1cnc(C)c(Nc2ncc3CC(=S)Nc4cc(ccc4-c3n2)C(F)(F)F)c1
• Target: PLK
• Solubility: DMSO:90 mg/mL (184.97 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.78 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PLK1:2 nM
• In Vivo:
  MLN0905 acts as a potent inhibitor of PLK1, exhibiting an IC50 value of 2 nM. It effectively hampers cell mitosis with an EC50 of 9 nM and inhibits cell proliferation in HT-29 cells, as evidenced by an LD50 of 22 nM. Furthermore, in a range of lymphoma cell lines, MLN0905 demonstrates the ability to diminish cell viability, with IC50 values ranging from 3 to 24 nM.
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• In Vitro:
  In nude mice bearing HT-29 xenografts, oral administration of MLN0905 (6.25 mg / Kg-50 mg / Kg) demonstrated a dose-dependent pharmacological response 48 hours post-treatment. Similarly, in mice harboring OCI LY-19-Luc tumors, oral MLN0905 (3.12 mg / Kg-6.25 mg / Kg) showed a pharmacological response 8 hours after treatment.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, MLN0905, MLN-0905, MLN 0905, PLK, PLK1, PLK1 Inhibitor, Polo-like Kinase (PLK)

Compound Identifiers

PubChem CID

46235922