JND3229

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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.

Western Blot AnalysisCell Line:BaF3 cells (overexpressing EGFRL858R/T790M/C797S or EGFR19D/T790M/C797S) Concentration:0.1, 0.3, 1, 3, 10 μM Incubation Time:2 h Result:Significantly inhibited the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in a dose-dependent manner.

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.

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Angiogenesis

EGFR

EGFR

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2260886-64-2

617.18

C33H41ClN8O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 12.5 mg/mL (20.25 mM; 超声助溶 )

CCC(=O)N[C@H]1CC[C@@H](CC1)N1C(=O)N(Cc2cnc(Nc3ccc(N4CCN(C)CC4)c(C)c3)nc12)c1ccccc1Cl

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(-20℃)

With Ice Pack

≥ 2 years