Vamotinib

SKU: orb1686292

Description

Vamotinib (PF-114) is a specific, orally bioavailable tyrosine kinase inhibitor that potently targets both native and T315I-mutant BCR-ABL, inducing apoptosis. It is a valuable research tool for investigating drug-resistant Ph+ leukemias and has been explored in preclinical models of Alzheimer's disease.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1416241-23-0
• MW: 532.56
• Purity: 99.83% (May vary between batches)
• Formula: C₂₉H₂₇F₃N₆O
• SMILES: CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3nnc4ccccn34)cc2C(F)(F)F)CC1
• Target: Tyrosine Kinases,Bcr-Abl,Apoptosis
• Solubility: 10% DMSO+90% Saline:2 mg/mL (3.76 mM);DMSO:30 mg/mL (56.33 mM)

Bioactivity

• Target IC50:
  Abl (Q252H):12 nM|Abl (H396P):1.0 nM|Abl (E255K):9.5 nM|Abl (Y253F):4.1 nM|Abl (T315I):0.78 nM|Abl (G250E):7.4 nM|BCR-ABL:0.49 nM|Abl (F317I):2.0 nM
• In Vivo:
  In female BALB/cAnNRj-Foxn1nu mice (K562 nude mouse xenograft model), Vamotinib (25/40 mg/kg, oral gavage; 14 days) resulted in a 100% reduction in average tumor volume within 4 weeks.
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• In Vitro:
  Vamotinib (0-1000 nM) inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner. Additionally, it can suppress the growth of Ph+ patient-derived cell lines, including K562, KCL-22, SupB15, Tom-1, BV-173, as well as Ph+ PD-LTC cells with non-mutated resistance and T315I mutation.
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Storage & Handling

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

Alternative Names

Bcr-Abl, BcrAbl, Apoptosis, PF-114, Tyrosine Kinases, TyrosineKinases

Compound Identifiers

PubChem CID

71475839