Dofequidar fumarate

SKU: orb1309752

Description

Dofequidar fumarate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 153653-30-6
• MW: 597.66
• Purity: 99.93%
• Formula: C₃₄H₃₅N₃O₇
• SMILES: OC(=O)\C=C\C(O)=O.OC(COc1cccc2ncccc12)CN1CCN(CC1)C(=O)C(c1ccccc1)c1ccccc1
• Target: P-gp
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.69 mM);H2O:1 mg/mL (1.67 mM);DMSO:100 mg/mL (167.32 mM)

Bioactivity

• In Vivo:
  Docetaxel alone at the maximum tolerated dose (MTD) has significant antitumor activity against intrinsically resistant HCT-15 tumor xenografts, while Dofequidar fumarate also enhances the antitumor effect of docetaxel active. For MCF-7/ADM tumor xenografts expressing large amounts of P-gp, docetaxel alone did not show antitumor activity at MTD, while the combination of MTD and Dofequidar fumarate for docetaxel greatly reduced MCF -7/ADM tumor growth. Intravenous injection of SBC-3 or SBC-3/ADM cells will produce metastatic colonies in the liver, kidneys, and lymph nodes in severe combined immunodeficiency (SCID) mice depleted by natural killer (NK) cells, although SBC-3/ ADM cells produce faster transfers than SBC-3 cells. The treatment of VP-16 and ADM reduced the formation of metastasis of SBC-3 cells, while the same treatment did not affect the metastasis of SBC-3/ADM cells. Although the use of MS-209 alone has no effect on the transfer of SBC-3 or SBC-3/ADM cells, the combined use of MS-209 and VP-16 or ADM can significantly inhibit the proliferation of SBC-3/ADM cells Metastasis to form an organ.
• In Vitro:
  Dofequidar fumarate effectively overcomes docetaxel resistance in MDR cancer cells, and this concentration reaches> 7 h in plasma without severe toxicity.Dofequidar fumarate restored the chemical sensitivity of SBC-3/ADM cells to VP-16, ADM and VCR in a dose-dependent manner in vitro. Dofequidar inhibits the outflow of chemotherapy drugs and increases the sensitivity of anti-cancer drugs to CSC-like side population (SP) cells isolated from various cancer cell lines. Dofequidar treatment greatly reduces the number of cells in the SP component. In 4-1St cells with strong resistance to ADM and VCR, Dofequidar fumarate at a concentration of 3 microM increased the cytotoxicity of ADM and VCR by 88-fold and 350-fold, respectively.

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

CD243, Cluster of differentiation 243, Dofequidar, Dofequidar fumarate, Dofequidar Fumarate, ABCB1, MS209, MS-209, MS 209, Multidrug resistance protein 1, Inhibitor, inhibit, MDR1, Pgp, P-glycoprotein, P-gp

Compound Identifiers

PubChem CID

9960287