Rezivertinib
CAS No. 1835667-12-3
Rezivertinib( —— )
Catalog No. M34868 CAS No. 1835667-12-3
Rezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 35 | In Stock |
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| 5MG | 132 | In Stock |
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| 10MG | 186 | In Stock |
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| 25MG | 345 | In Stock |
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| 50MG | 482 | In Stock |
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| 100MG | 693 | In Stock |
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| 200MG | 918 | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameRezivertinib
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NoteResearch use only, not for human use.
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Brief DescriptionRezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.
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DescriptionRezivertinib (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.
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In VitroRezivertinib (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).
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In VivoRezivertinib (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).
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Synonyms——
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PathwayAngiogenesis
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TargetEGFR
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RecptorEGFR
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Research Area——
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Indication——
Chemical Information
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CAS Number1835667-12-3
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Formula Weight486.57
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Molecular FormulaC27H30N6O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 125 mg/mL (256.90 mM; Ultrasonic )
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SMILESO=C(C=C)NC1=CC(NC=2N=CC=C(N2)C3=CN(C=4C=CC=CC34)C)=C(OC)C=C1OCCN(C)C
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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Olmutinib
Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.?
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AV-412
AV-412 is an EGFR inhibitor (EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M and ErbB2 with IC50s of 0.75, 0.79, 0.5, 2.3, 19 nM).In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.?
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Lazertinib
Lazertinib (YH25448, GNS-1480) is a highly potent, mutant-selective, irreversible, brain-penetrant and orally active EGFR tyrosine-kinase inhibitors for both the T790M mutation and activating EGFR mutations.
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