Bafetinib

SKU: orb1223834

Description

A potent and selective dual Abl/Lyn tyrosine kinase inhibitor with IC50 of 5.9 nM and 198 nM, respectively; more potent and specific against Bcr-Abl than imatinib, also inhibits the phosphorylation of CrkL and ERK in BaF3/E255K cells; inhibits the phosphorylation of Bcr-Abl harboring the M244V, G250E, Q252H, Y253F, E255K, E255V, F317L, M351T, E355G, F359V, H396P, or F486S mutations, but does not inhibit the phosphorylation of the T315I mutant; prolonges the survival of mice injected with leukemic cells expressing all mutated Bcr-Abl.Blood Cancer Phase 2 Clinical.

Key Properties

• CAS Number: 859212-16-1
• MW: 576.6154
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₁F₃N₈O
• SMILES: O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CN=CN=C3)=N2)=C1)C4=CC=C(CN5C[C@@H](N(C)C)CC5)C(C(F)(F)F)=C4
• Target: Bcr-Abl
• Solubility: DMSO: ≥ 42 mg/mL

Bioactivity

• In Vivo:
  Animal model: Murine inflammatory pain model. Dosage: 10 mg/kg. Administration: i. g. Result: Inhibited PAR2-induced mechanical hyperalgesia.
• In Vitro:
  Western blot analysis. Cell line: H292. Concentration: 0.625, 1.25, 2.5 μM Incubation time: 24 h. Result: Inhibited the expression of PD-L1 and c-Myc.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

INNO-406 | NS-187

Quick Database Links

Gene Symbol

Bcr-Abl