EGFR-IN-206 

EGFR-IN-206 is an orally active EGFR inhibitor. EGFR-IN-206 inhibits the phosphorylation of the key tumor growth protein EGFR, and suppresses the proliferation, migration and invasion of EGFR triple-mutant tumor cell lines. EGFR-IN-206 downregulates the expression of inflammation-related proteins iNOS, COX-2 and NF-κB (p65). EGFR-IN-206 promotes the secretion of NO. EGFR-IN-206 reduces the secretion of IL-6. EGFR-IN-206 induces apoptosis (apoptosis) of EGFR triple-mutant tumor cells. EGFR-IN-206 exerts antitumor activity in EGFR triple-mutant mice. EGFR-IN-206 is applicable to the research of non-small cell lung cancer^[1].

EGFR-IN-206 (Compound 9f) 可强效抑制三种 EGFR 三重突变癌细胞系的增殖，包括 Baf3-EGFR^{L858R/C797S/T790M} (IC₅₀ = 33.3 nM)、Baf3-EGFR^{Del19/C797S/T790M} (IC₅₀ = 35.8 nM) 和 H1975-EGFR^{L858R/C797S/T790M} (IC₅₀ = 95.3 nM)^[1]。
EGFR-IN-206 (10-50 nM, 24 h) 抑制 Baf3-EGFR^{L858R/C797S/T790M} 细胞和 H1975-EGFR^{L858R/C797S/T790M} 细胞的迁移与侵袭^[1]。
EGFR-IN-206 (50-500 nM) 可剂量依赖性地增加 H1975-EGFR^{L858R/C797S/T790M} 3D 球状体中的死细胞占比^[1]。
EGFR-IN-206 (10-1000 nM) 以剂量依赖的方式降低 Baf3-EGFR^{L858R/C797S/T790M} 和 H1975-EGFR^{L858R/C797S/T790M} 细胞的线粒体膜电位，促进细胞凋亡，升高细胞内的活性氧水平^[1]。
EGFR-IN-206 (10-1000 nM) 可剂量依赖性地抑制 H1975-L858R/C797S/T790M 细胞中 EGFR 的磷酸化，且不改变总 EGFR 的表达水平^[1]。
EGFR-IN-206 抑制 LPS (HY-D1056) 刺激的 Raw264.7、THP-1 细胞中 NO 的分泌，其 EC₅₀ 分别为 101.4、144.7 nM^[1]。
EGFR-IN-206 (10-50 nM; 12 h) 可显著降低经 LPS 刺激的 Raw264.7 和 THP-1 细胞孵育 12 h 后的 IL-6 分泌水平、iNOS、COX-2 和 NF-κB (p65) 的表达^[1]。
EGFR-IN-206 (50-100 nM) 在 50 nM 浓度下可在 THP-1 共培养模型中抑制 H1975-L858R/C797S/T790M 细胞经炎症增强的集落形成能力，减少 IL-6 的分泌^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EGFR-IN-206 (50 mg/kg；口服；每日 1 次；连续 7 天) 在携带有 EGFR^{L858R/T790M/C797S} 三重突变 H1975 肿瘤的裸鼠中实现了 67.3%的肿瘤生长抑制率，同时瘤内 p-EGFR 和 COX-2 的表达水平降低^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

617.76

C₃₂H₃₉N₇O₄S

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Tan Z, et al. Synthesis and evaluation of methoxyquinazoline sulfonamide derivatives as bifunctional molecular targeting tumor related inflammation and anti-EGFR triple-mutation. Bioorg Chem. 2026;173:109624.  [Content Brief]