| Name | BLU-945 |
| Description | BLU-945 is a reversible, potent, highly selective, and orally available epidermal growth factor receptor tyrosine kinase inhibitor (TKIs). BLU-945 inhibits EGFR phosphorylation in EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S mutant cell lines. BLU-945 can be used in lung cancer research, including non-small cell lung cancer (NSCLC). |
| 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)[1]；BLU-945 (1-10000μM) inhibits EGFR phosphorylation in EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S mutant cell lines. [3] |
| 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. [1] |
| 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. |
| Solubility Information | DMSO : 100 mg/mL (179.6 mM), Sonication and heating to 60℃ are recommended.
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| Keywords | BLU-945 |
| Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
