产品
编 号:F282406
分子式:C33H41ClN8O2
分子量:617.18
产品类型
结构图
CAS No: 2260886-64-2
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产品详情
生物活性:
JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.
体内研究:
JND3229 (10 mg/kg;腹腔注射;每天两次,持续 10 天) 表现出明显的肿瘤生长抑制作用,并在体内表现出靶向抑制作用。Animal Model:BALB/c mice (bearing established BaF3-EGFR19D/T790M/C797S mouse xenograft tumors model).
Dosage:10 mg/kg
Administration:Intraperitoneal injection; twice daily for 10 days.
Result:Caused an obvious suppression of tumor growth with a Tumor Growth Inhibition (TGI) value of 42.2%.Showed well tolerance without obvious body weight loss or other obvious toxic sign in the treated animals.Significantly decreased the level of phosphorylated EGFR (p-EGFR) tin the tumor tissues.
体外研究:
JND3229 有效抑制 BaF3 细胞 (携带 EGFRL858R/T790M/C797S 和 EGFR19D/T790M/C797S 突变)、NCI-H1975 NSCLC 细胞 (EGFRT790M 突变) 和 A431 癌细胞 (过表达 EGFRWT) 的 IC50 值分别为 0.51、0.32、0.31 和 0.27 μM。 JND3229 (0.1、0.3、1、3、10 μM;2 小时) 有效抑制 EGFRL858R/T790M/C797S 和 EGFR 的磷酸化>19D/T790M/C797S 在工程化 BaF3 电池中。