TAK-733

SKU: orb1300550

Description

TAK-733 is a selective, orally active MEK1/2 inhibitor used in cancer research. It has demonstrated antitumor activity in preclinical studies, inhibiting tumor growth in various in vivo models and cell proliferation in vitro, particularly within the MAPK/ERK pathway.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1035555-63-5
• MW: 504.23
• Purity: 99.53% (May vary between batches)
• Formula: C₁₇H₁₅F₂IN₄O₄
• SMILES: Cn1c2ncn(C[C@@H](O)CO)c(=O)c2c(Nc2ccc(I)cc2F)c(F)c1=O
• Target: MEK
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (6.54 mM);H2O:<1 mg/mL;Ethanol:<1 mg/mL;DMSO:93 mg/mL (184.44 mM)

Bioactivity

• Target IC50:
  MEK1:3.2 nM
• In Vivo:
  TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg.
• In Vitro:
  TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAK733, TAK-733, TAK 733, MEK1, MEK, MAP2K, MAPKK, Inhibitor, inhibit, Mitogen-activated protein kinase kinase

Compound Identifiers

PubChem CID

24963252