Rezivertinib hydrochloride  (Synonyms: BPI-7711 hydrochloride)

Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC)^[1][2].

Rezivertinib (BPI-7711) hydrochloride 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) hydrochloride shows significant tumor regression^[2].
Rezivertinib (12.5 mg/kg/day; orally; 14 days) hydrochloride survives an average of 112% longer in H1975-luc human NSCLC mice model^[2].
Rezivertinib (50 mg/kg/day; orally) hydrochloride has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

523.03

C₂₇H₃₁ClN₆O₃

2170255-78-2

O=C(NC1=CC(NC2=NC(C3=CN(C)C4=C3C=CC=C4)=CC=N2)=C(C=C1OCCN(C)C)OC)C=C.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.