Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 5 mg | In stock | $ 289 | |
| 10 mg | In stock | $ 549 | |
| 20 mg | In stock | $ 785 | |
| 50 mg | In stock | $ 1588 | |
| 100 mg | In stock | $ 2382 |
| Description | Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants. |
| Targets&IC50 | TrkA:0.622 nM, TrkB:2.28 nM, ROS1:0.207 nM, TrkC:0.980 nM |
| In vitro | The IC50 of Taletrectinib (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells is ~3-20 nM.Taletrectinib (0.001-1000 nM; 2 hours) dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells in vitro.Taletrectinib potently inhibits autophosphorylation of ROS1 in JFCR-165, JFCR-168, and MGH193-1B cells.Taletrectinib partially suppresses phospho-NTRK1 at 10 nM, and completely suppresses by 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in an ATP-competitive manner. Taletrectinib almost completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but did not inhibit other 152 kinases strongly. Taletrectinib effectively inhibits Crizotinib-resistant ROS1 secondary mutations, including G2032R solvent front mutation. |
| In vivo | Taletrectinib (DS-6051b) (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity.Taletrectinib (6.25-200 mg/kg; p.o.; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice bearing KM12 cells.Taletrectinib (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in the wild-type (WT) and the G2032R-mutant Ba/F3-bearing mice without severe body weight loss. |
| Synonyms | AB-106, DS-6051b |
| CAS No. | 1505515-69-4 |
| Chemical Formula | C29H34FN5O5 |
| Molecular Weight | 551.619 |
| Solubility | DMSO: 50 mg/mL (90.64 mM), Need ultrasonic |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
In vivo Formulation Calculator (Clear solution)Calculatorbottom
