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DBPR112
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DBPR112图片
CAS NO:1226549-49-0
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
DBPR112 是一种口服有效的基于氟嘧啶的 EGFR 抑制剂,对 EGFRWT 和 EGFRL858R/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。

产品描述

DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.

体外活性

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].

体内活性

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[1]. DBPR112 (IV; 5 mg/kg) has a T1/2 of 2.3 hours, a CL of 55.6 mL/minokg, and a Vss of 8.6 L/kg for rats[1].

Cas No.

1226549-49-0

分子式

C32H31N5O3

分子量

533.62

别名

DBPR112

储存和溶解度

DMSO:225mg/mL (421.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years