DBPR112

SKU: orb1709923

Description

DBPR112 is an orally bioavailable furanopyrimidine inhibitor targeting the EGFR ATP-binding site, demonstrating potent activity against wild-type (IC50=15 nM) and L858R/T790M mutant (IC50=48 nM) forms. It has shown significant antitumor efficacy in preclinical research models, supporting its investigation in oncology studies for EGFR-driven cancers.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1226549-49-0
• MW: 533.62
• Purity: 99.25%
• Formula: C₃₂H₃₁N₅O₃
• SMILES: CN(C)C\C=C\C(=O)Nc1cccc(c1)-c1c(oc2ncnc(N[C@H](CO)c3ccccc3)c12)-c1ccccc1
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.37 mM);DMSO:225 mg/mL (421.65 mM)

Bioactivity

• Target IC50:
  EGFR (WT):15 nM|EGFR (L858R/T790M):48 nM
• 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 . 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 .
• In Vitro:
  DBPR112 (0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner. DBPR112 shows the inhibitory activity against HCC827 (CC50=25 nM), H1975 (CC50=620 nM) and A431 Cell (CC50=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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DBPR112, DBPR-112, DBPR 112, EGFR (wt), EGFR (L858R/T790M), EGFRL858R/T790M, EGFRWT

Compound Identifiers

PubChem CID

46212971