Rezivertinib (Synonyms: BPI-7711) |
| Catalog No.GC62341 |
레지베르티닙(BPI-7711)은 경구 활성, 고도로 선택적이고 비가역적인 3세대 EGFR 티로신 키나제 억제제(TKI)입니다. 레지베르티닙은 일반적인 활성화 EGFR 및 내성 T790M 돌연변이에 대해 높은 효능을 나타냅니다. 레지버티닙은 중추신경계(CNS) 침투가 우수하고 항종양 활성이 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1835667-12-3
Sample solution is provided at 25 µL, 10mM.
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Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity[1][2].
Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI50 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and > 1000 nM (A431, EGFR WT)[1].
Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression[2]. Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model[2]. Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days)[2].
[1]. Misako Nagasaka, et al. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2021 May;16(5):740-763.
[2]. Victoria L. Wilde, et al. Preclinical evidence of BPL-7711 activity in Egfr-mutant non-smallcell lung cancer ( NSCLC ) in orthotopically implanted human tumorxenografts in the lung and brain.
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