Rezivertinib hydrochloride
Based on 1 publication(s) in Google Scholar
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).
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- CAS No.: 2170255-78-2
- Formule: C27H31ClN6O3
- Masse moléculaire:523.03
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Rezivertinib hydrochloride
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Activité biologique
Description
In Vitro
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. Further protocols information, click here.
In Vivo
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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2170255-78-2
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Masse moléculaire 523.03
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Formule C27H31ClN6O3
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SMILES
O=C(NC1=CC(NC2=NC(C3=CN(C)C4=C3C=CC=C4)=CC=N2)=C(C=C1OCCN(C)C)OC)C=C.Cl
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Synonyms
BPI-7711 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Protocole
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rezivertinib hydrochloride Related Classifications
HY-109189A Related Classifications
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