Potent dual MCT1/2 inhibitor; orally bioavailable
BAY 8002 is a potent dual MCT1/2 inhibitor (IC50 values are 3, 8, and 12 nM at rat (C6), human (DLD-1) and mouse (4T1) MCT1 respectively; IC50 values of human MCT1, MCT2, and MCT4 isoforms recombinantly expressed in
X. laevis
oocytes are 1, 5 and >500 nM, respectively); suppresses bidirectional lactate transport. Inhibits cellular SNARF-5 fluorescence change (IC50 = 85 nM) in MCT1-expressing DLD-1 cells. Arrests growth and increases intratumor lactate levels of Raji tumor xenografts in mice. Orally bioavailable.
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-151783 |
| Réf. fabricant | 18775606 |
| Quantité | 10 mg |
| Formule moléculaire | C<sub>20</sub>H<sub>14</sub>ClNO<sub>5</sub>S |
| Poids de la formule | 415.85 |
| Type de produit | Inhibitor |
| Pureté | 98% |
