BLU-945

SKU: orb1685231

Description

BLU-945 is a selective, oral EGFR tyrosine kinase inhibitor designed to target resistant mutations like L858R/T790M/C797S. It is a research tool for studying non-small cell lung cancer (NSCLC), demonstrating activity in both in vitro cell line models and in vivo studies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2660250-10-0
• MW: 556.7
• Purity: 99.16% (May vary between batches)
• Formula: C₂₈H₃₇FN₆O₃S
• SMILES: CO[C@@H]1CCN(C[C@@H]1F)c1nccc(Nc2cc3c(ccc(N4C[C@H](CS(C)(=O)=O)[C@H]4C)c3cn2)C(C)C)n1
• Target: EGFR
• Solubility: DMSO:250 mg/mL (449.07 mM)

Bioactivity

• In Vivo:
  METHODS: BLU-945 (30, 100 mg/kg, twice daily) was administered to mice bearing NCI-H1975 xenografts. RESULTS BLU-945 at 100 mg/kg induced tumor stasis in mice bearing NCI-H1975 xenografts.
• In Vitro:
  BLU-945 exhibits subnanomolar activity against EGFR+/T790M and EGFR+/T790M/C797S mutants and maintains activity against EGFR activating mutations (L858R, ex19del), especially EGFR L858R; BLU-945 exhibits excellent inhibitory activity against the pEGFR H1975 cell line (IC50 = 1.1 nM), which is approximately 500-fold more potent than pEGFR A431 (EGFR-WT amplified cell line); in addition, BLU-945 can effectively inhibit EGFR phosphorylation in the Ba/F3 engineered cell line (L858R/T790M/C797S IC50 = 3.2 nM, ex19del/T790M/C797S IC50 = 4.0 nM)；BLU-945 (1-10000μM) inhibits EGFR phosphorylation in EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S mutant cell lines.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EGFR, BLU945, BLU-945, BLU 945

Compound Identifiers

PubChem CID

156538665