JND3229 是一种可逆性的 EGFRC797S 抑制剂，对 EGFRL858R/T790M/C797S、EGFRWT 和 EGFRL858R/T790M 的 IC50 值分别为 5.8、6.8 和 30.5 nM。JND3229 具有较好的抗增殖活性，能有效地抑制体内肿瘤的生长。JND3229 可用于癌症，尤其是非小细胞癌的研究。

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.

JND3229 potently inhibits the proliferation of BaF3 cells (harboring the EGFRL858R/T790M/C797S and EGFR19D/T790M/C797Smutations), NCI-H1975 NSCLC cells (with EGFRT790M mutation) and A431 cancer cells (overexpressing EGFRWT) with IC50 values of 0.51, 0.32, 0.31 and 0.27 μM, respectively. JND3229 (0.1, 0.3, 1, 3, 10 μM; 2 h) potently inhibits the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in engineering BaF3 cells[1].

JND3229 (10 mg/kg; i.p.; twice daily for 10 days) exhibits an obvious suppression of tumor growth, and shows target inhibition in vivo[1].

2260886-64-2

C33H41ClN8O2

617.18

DMSO:11.7mg/mL (19mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years