| Bioactivity | D6808 is a highly selective and potent c‑Met inhibitor with an IC50 value of 2.9 nM. D6808 induces cell apoptosis and cell cycle arrest. D6808 can be used for the research of NSCLC and gastric cancers[1]. |
| Target | IC50: 2.9 nM (c‑Met) |
| Invitro | D6808 shows c-Met biochemical kinase inhibitory activity with an IC50 value of 2.9 nM[1].D6808 (0.0001-10 μM; 5 d) shows cellular antiproliferative potency to Hs746T cancer cells with an IC50 value of 0.7 nM[1].D6808 displays extraordinary kinome selectivity with IC50 values of 401.3, 437.2, 1386 and 203.9 nM for Axl, TrkA, TrkB and TrkC kinase, respectively[1].D6808 (0-10 μM; 72 h) show antiproliferative potency to Tpr-Met fusion protein-transformed Ba/F3 cells with IC50 values of 4.3, 4.2, 3.2, 1.0, 39.0 and 33.4 nM for Ba/F3-Tpr-Met, Ba/F3-Tpr-MetF1200L, Ba/F3-Tpr-MetM1250T, Ba/F3-Tpr-MetH1094Y, Ba/F3-Tpr-MetF1200I, Ba/F3-Tpr-MetL1195V, respectively[1].D6808 (0-30 nM; 12 h) affects activation of MET and dose-dependently decreases the protein levels of CDK2, CDK4, CDK6, cyclin D2, and cyclin E1 and the cleave activation of PARP and caspase-9 in Ba/F3-Tpr-Met cells[1].D6808 (40 nM; 24 h) induces cell apoptosis and 87.37% G0/G1 phase arrest in Ba/F3-Tpr-Met cells[1]. Cell Proliferation Assay[1] Cell Line: |
| In Vivo | 1.19Pharmacokinetic Properties of D6808 in Rats[1]. |
| Name | D6808 |
| Formula | C30H25F3N6O2 |
| Molar Mass | 558.55 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Wang C, et al. Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring MET Gene Alteration Treatment. J Med Chem. 2022 Nov 24;65(22):15140-15164. |