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Rezivertinib

Catalog No. T36644 CAS 1835667-12-3

Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2].

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Rezivertinib, CAS 1835667-12-3

Pack Size	Availability	Price/USD
5 mg	6-8 weeks	$ 297.00
25 mg	6-8 weeks	$ 916.00
50 mg	6-8 weeks	$ 1,190.00
100 mg	6-8 weeks	$ 1,860.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2].
In vitro	Rezivertinib (BPI-7711) effectively inhibits the proliferation of cells with EGFR mutations, demonstrating selective activity across various cell lines with GI50 values of 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), and 22 nM (NCI-H1975, del19/T790M), while showing minimal effect on cells expressing wild-type EGFR with a GI50 of >1000 nM (A431, EGFR WT)[1].
In vivo	Rezivertinib (BPI-7711; orally administered at dosages ranging from 6.25 to 25 mg/kg/day over a period of 14 days) demonstrates significant tumor regression[2]. When given at a concentration of 12.5 mg/kg/day for the same duration, it results in a 112% increase in the average lifespan of mice in the H1975-luc human NSCLC model[2]. At a higher dosage of 50 mg/kg/day, Rezivertinib exhibits anti-tumor effectiveness, leading to an average survival extension of the test animals by 115% (comparing 28 days to 13 days)[2].

Molecular Weight	486.57
Formula	C27H30N6O3
CAS No.	1835667-12-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (256.90 mM), Sonication is recommended.

References and Literature

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.

Dose Conversion

You can also refer to dose conversion for different animals. More

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Rezivertinib 1835667-12-3 inhibitor inhibit

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