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DBPR112

CAS No. : 1226549-49-0

MCE 国际站：DBPR112

产品活性：DBPR112 是一种口服有效的基于氟嘧啶的 EGFR 抑制剂，对 EGFR^WT 和 EGFR^L858R/T790M 的 IC₅₀ 分别为 15 nM 和 48 nM。DBPR112 可以占据 ATP 结合位点。DBPR112 具有显着的抗肿瘤功效。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

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 (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.

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.

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