| Name | DBPR112 |
| Description | DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM for EGFRWT and 48 nM for EGFRL858R/T790M, capable of occupying the ATP-binding site and demonstrating significant antitumor efficacy. |
| In vitro | DBPR112 (0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner[1]. DBPR112 shows the inhibitory activity against HCC827 (CC50=25 nM), H1975 (CC50=620 nM) and A431 Cell (CC50=1.02 μM) cell lines[1]. 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[1]. |
| In vivo | DBPR112 administered orally at 20-50 mg/kg for 5 days per week over 2 weeks significantly reduces tumor growth in the HCC827 tumor model. Oral administration of DBPR112 at 50 mg/kg once daily for 15 days results in a mean tumor growth inhibition of 34% in the H1975 tumor model [1]. Intravenous administration of DBPR112 at 5 mg/kg in rats shows a T1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a Vss of 8.6 L/kg [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (9.37 mM), Sonication is recommended.
DMSO : 150 mg/mL (281.1 mM), Sonication is recommended.
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| Keywords | EGFRWT | EGFRL858R/T790M | EGFR (wt) | EGFR (L858R/T790M) | DBPR-112 | DBPR112 | DBPR 112 |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
