Taletrectinib

• 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[1][2].

• Product Name Alternative:

  DS-6051b; AB-106; IBI-344

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  ROS Kinase

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/taletrectinib.html

• Purity:

  99.78

• Solubility:

  DMSO : 50 mg/mL (ultrasonic)

• Smiles:

  O=C(O)CCCCC(O)=O.C[C@@H](NC1=NN2C(C=C1)=NC=C2C3=CC=C(OC[C@H](N)C)C=C3)C4=CC=CC(F)=C4

• Molecular Formula:

  C29H34FN5O5

• Molecular Weight:

  551.61

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Katayama R, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10 (1) :3604. Published 2019 Aug 9.|[2]Fujiwara Y, et al. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018;9 (34) :23729-23737. Published 2018 May 4.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• CAS Number:

  [1505515-69-4]