Rezivertinib free base · Synonyms: BPI-7711

Rezivertinib is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

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Data Sheet SDS COA

Rezivertinib structure

CAS No.: 1835667-12-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 495.00	BP-01260-50mg	In stock	Get quote
100 mg	USD 780.00	BP-01260-100mg	In stock	Get quote
250 mg	USD 1,560.00	BP-01260-250mg	In stock	Get quote
500 mg	USD 2,500.00	BP-01260-500mg	In stock	Get quote
1 g	USD 3,950.00	BP-01260-1g	In stock	Get quote
2 g	Inquire	BP-01260-2g	In stock	Inquire
3 g	Inquire	BP-01260-5g	In stock	Inquire

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Description

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 .

Biological activity

In Vitro 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). In Vivo Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression. Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model. 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).

Identifiers

SMILES: C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1OCCN(C)C)=O
InChIKey: BPMZUKYFIDPLEA-UHFFFAOYSA-N

Specifications

MW (average): 486.5655
Formula: C₂₇H₃₀N₆O₃
CAS No.: 1835667-12-3
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

soluble in DMSO

Documents

References

[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.

Same target

Search EGFR

Same research area

Search Cancer