SPH5030_product_DataBase

Bioactivity	SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer[1].
Target	IC50: 3.51 nM (HER2WT), 0.42 nM (HER2D769H), 0.43 nM (HER2D769Y), 0.16 nM (HER2V777L), 0.56 nM (HER2R896C), 8.13 nM (EGFRWT)
Invitro	SPH5030 (0-10 μM; 72 h) shows anti-proliferation activities against tumor cell lines[1]. Cell Cytotoxicity Assay[1] Cell Line:
In Vivo	SPH5030 (5-40 mg/kg; p.o. once per day for 13 or 21 days) shows in vivo antitumor efficacy in mice with xenograft tumor models[1]. 1.19Pharmacokinetic Properties of SPH5030 in Mice and Rats[1].
Name	SPH5030
CAS	2364326-23-6
Formula	C31H31FN8O3
Molar Mass	582.63
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]. Li D,et al. Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment. J Med Chem. 2022 Apr 14;65(7):5334-5354.

PeptideDB