EGFR-IN-82_product_DataBase

Bioactivity	EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research [1].
Target	0.09 , 0.06 nM (EGFRL858R/T790M/C797S, EGFRDel19/T790M/C797S)
Invitro	EGFR-IN-82 (compound 8a) (72 h) 显著抑制 Ba/F3-EGFRDel19/T790M/C797S 细胞的生长，其 IC50 值为 12.7 nM，但对 A431 细胞的生长无显著作用[1]。 0 --> EGFR-IN-82 相关抗体:
In Vivo	EGFR-IN-82 (compound 8a) 体内药代动力学性能优于 Brigatinib (HY-12857)[1]。EGFR-IN-82 (15 - 30 mg/kg, 口服, 14 - 21 天) 中度抑制 PC9-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长，高度抑制 Ba/F3-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长[1]。在 Balb/C 小鼠中的药代动力学分析[1]Route
Name	EGFR-IN-82
CAS	2568086-81-5
Formula	C32H41BrN9O2P
Molar Mass	694.60
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. 1. Yanliang Guo, et al. Design, synthesis and biological evaluation of phosphoroxy quinazoline derivatives as potential EGFRT790M/C797S inhibitors. Bioorganic & Medicinal Chemistry. Volume 90, 15 July 2023, 117338.

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