ARQ 621

SKU: orb1300807

Description

ARQ 621 is a selective, allosteric inhibitor of the mitotic kinesin Eg5 (KIF11). It has been investigated in Phase 1 clinical studies for cancer and is used in preclinical research to study mitosis, aneuploidy, and tumor cell proliferation in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1095253-39-6
• MW: 552.43
• Purity: 98.38% (May vary between batches)
• Formula: C₂₈H₂₄Cl₂FN₅O₂
• SMILES: NCCCN([C@H](CC#C)c1nc2cc(Cl)ccc2c(=O)n1Nc1ccccc1)C(=O)c1cccc(Cl)c1F
• Target: Kinesin
• Solubility: Ethanol:93 mg/mL (168.35 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (168.35 mM)

Bioactivity

• In Vivo:
  ARQ 621, as a novel clinical stage drug candidate, inhibits a number of xenografts grown in athymic mice, such as pancreatic, breast, prostate, and ovarian carcinomas with no hematological changes. Furthermore, for ARQ 621, there is no envidence of bone marrow toxicity in pre-clinical mouse efficacy models or safety studies in rats and dogs.
• In Vitro:
  ARQ 621 demonstrates anti-tumor activity against a wide range of human cancer cell lines in vitro, including colon, lung, endometrial, bladder, and hematologic cancer cell lines, with significantly less cytotoxicity against hematopoietic cells.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | 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

cell, division, Anti-tumor, ARQ 621, ARQ621, ARQ-621, microtubule, Kinesin, inhibit, motor, Inhibitor, Eg5 mitotic motor protein, Eg5, protein

Compound Identifiers

PubChem CID

25110841