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BLU-945

🥰Excellent
Catalog No. T9754Cas No. 2660250-10-0
Alias BLU945, BLU 945

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).

BLU-945

BLU-945

🥰Excellent
Purity: 99.16%
Catalog No. T9754Alias BLU945, BLU 945Cas No. 2660250-10-0
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 SizePriceAvailabilityQuantity
1 mg$97In Stock
5 mg$214In Stock
10 mg$320In Stock
25 mg$546In Stock
50 mg$819In Stock
100 mg$1,258In Stock
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Purity:99.16%
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Product Introduction

Bioactivity
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]
AliasBLU945, BLU 945
Chemical Properties
Molecular Weight556.7
FormulaC28H37FN6O3S
Cas No.2660250-10-0
SmilesCO[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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.7963 mL8.9815 mL17.9630 mL89.8150 mL
5 mM0.3593 mL1.7963 mL3.5926 mL17.9630 mL
10 mM0.1796 mL0.8981 mL1.7963 mL8.9815 mL
20 mM0.0898 mL0.4491 mL0.8981 mL4.4907 mL
50 mM0.0359 mL0.1796 mL0.3593 mL1.7963 mL
100 mM0.0180 mL0.0898 mL0.1796 mL0.8981 mL

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