DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC 50 s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M , respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.
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Product Description
DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC 50 s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M , respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy
In Vitro
DBPR112 (compound 78; 0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner. DBPR112 shows the inhibitory activity against HCC827 (CC 50 =25 nM), H1975 (CC 50 =620 nM) and A431 Cell (CC 50 =1.02 μM) cell lines. DBPR112 occupies the ATP-binding site and interacts with surrounding residues by covalent bonding, hydrogen bonds, and hydrophobic interactions, which give it a potent inhibitory activity against WT EGFR. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: H1975 cells Concentration: 0.32, 1.6, 8.0, 40, 200, 1000 nM Incubation Time: 16 hours Result: Induced reduction of phosphorylated EGFR in a dose-dependent manner in H1975 cells.
In Vivo
DBPR112 (orally; 20-50 mg/kg; 5 days/week for 2 consecutive weeks) significantly reduces tumor growth in HCC827 tumor model. DBPR112 (orally; 50 mg/kg; once a day for 15 days) has a significant antitumor effect (mean tumor growth inhibition of 34%) in H1975 tumor model . DBPR112 (IV; 5 mg/kg) has a T 1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a V ss of 8.6 L/kg for rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice) Dosage: 20, 50 mg/kg Administration: Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12) Result: Significantly reduced tumor growth. Animal Model: Rats Dosage: 5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a V ss of 8.6 L/kg by IV. Had a T 1/2 of 3.4 hours, a C max of 508 ng/mL and an AUC of 2978 ng/mL•h by PO.
This compound belongs to the class of organic compounds known as 2,3-diphenylfurans. These are organic heterocyclic compounds that contain a furan ring substituted with a phenyl group only the C2- and C3-positions.
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1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
