Tafetinib

SKU: orb1699186

Description

Tafetinib (SIM-010603) is a potent, orally bioavailable tyrosine kinase inhibitor demonstrating anti-angiogenic and anti-tumor properties. It has shown efficacy in preclinical in vitro cell proliferation assays and in vivo xenograft models, supporting its investigation in oncology research, particularly for solid tumors.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1032265-57-8
• MW: 424.51
• Purity: 96.78% (May vary between batches)
• Formula: C₂₄H₂₉FN₄O₂
• SMILES: O=C1/C(=C/2\C3=C(C(C(NCCN(CC)CC)=O)=C(C)N3)CCC2)/C=4C(N1)=CC=C(F)C4
• Target: c-Kit,VEGFR,c-RET,Tyrosine Kinases
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• In Vivo:
  Tafetinib, a promising multi-targeted receptor tyrosine kinase (RTK) inhibitor, is now being considered for evaluation in a phase clinical trial. In this work, the subchronic toxicity of Tafetinib in SD rats and beagle dogs has been characterized. Rats and dogs received Tafetinib orally (0-20 and 0-10mg/kg/day, respectively) on a consecutive daily dosing schedule for 28 days following a 14-day recovery period. Sunitinib was used as a positive control. The No Observed Adverse Effect Level (NOAEL) of Tafetinib was 5mg/kg/day for rats, and undefined for dogs. The treatment resulted in unscheduled mortality in dogs receiving 10mg/kg of Tafetinib or Sunitinib. The adverse effects of Tafetinib on rats and dogs mainly included gastrointestinal toxicity, skeletal toxicity, myelosuppression, thymus atrophy, bronchopneumonia, cardiovascular dysfunction, and pancreatic toxicity. Similar observations have also been noted with this class of RTK signaling inhibitors and are consistent with pharmacologic perturbations of physiologic/angiogenic processes associated with the intended molecular targets. Most treatment-induced effects were reversible or showed ongoing recovery upon discontinuation of treatment. Tafetinib has shown a comparable toxicity effect on beagle dogs, while better tolerability on SD rats when compared to Sunitinib.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tafetinib, SIM010603, SIM-010603, SIM 010603, TyrosineKinases, Tyrosine Kinases

Compound Identifiers

PubChem CID

56935577