BLU-945 是一种强效的、高选择性的、口服有效的、可逆的表皮生长因子受体酪氨酸激酶抑制剂 (TKIs)。BLU-945 可有效抑制具有 L858R 和/或外显子 19 缺失突变、T790M 突变和 C797S 突变的 EGFR。BLU-945 可用于肺癌包括非小细胞肺癌（NSCLC）的研究。

BLU-945 is a potent, highly selective, reversible and orally active inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC).

BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants, IC50 value range from 1.2-4.4 nM[2]. BLU-945 (0- 10 mM, 4 h) inhibit EGFR phosphorylation in the EGFR L858R/T790M/C797S, and EGFR ex19del/T790M/C797S mutant cell lines[2].

BLU-945 (oral, 0-100 mg/kg; bid) shows potent, robust EGFR pathway inhibition and anti-tumor activity in triple-mutant osimertinib-resistant Ba/F3 CDX and PDCX models[2].

2660250-10-0

C28H37FN6O3S

556.7

BLU945;BLU 945

DMSO:100 mg/mL (179.6 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years