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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $97 | In Stock | |
5 mg | $214 | In Stock | |
10 mg | $320 | In Stock | |
25 mg | $546 | In Stock | |
50 mg | $819 | In Stock | |
100 mg | $1,258 | In Stock |
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] |
Alias | BLU945, BLU 945 |
Molecular Weight | 556.7 |
Formula | C28H37FN6O3S |
Cas No. | 2660250-10-0 |
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 |
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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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