BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). 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).
性状
Solid
体外研究(In Vitro)
BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants with IC50 value range from 1.2-4.4 nM.BLU-945 (0- 10 mM, 4 h) inhibit EGFR phosphorylation in the EGFR L858R/T790M/C797S, and EGFR ex19del/T790M/C797S mutant cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
BLU-945 (oral, 0-100 mg/kg; bid) demonstrates potent, robust EGFR pathway inhibition and anti-tumor activity in triple-mutant osimertinib-resistant Ba/F3 CDX and PDCX models. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
ClinicalTrial
参考文献
[1]. John Emmerson Campbell, et al. Inhibitors of mutant forms of egfr. Patent WO2021133809A1.[2]. Sun Min Lim, et al. BLU-945, a fourth-generation, potent and highly selective epidermal growth factor receptor tyrosine kinase inhibitor with intracranial activity, demonstrates robust in vivo anti-tumor activity in models of osimertinib-resistant non-sma[3]. Meredith S Eno, et al. Discovery of BLU-94
溶解度数据
In Vitro: DMSO : 125 mg/mL (224.54 mM; ultrasonic and warming and heat to 60°C)配制储备液