EGFR inhibitor

SI-8033

EGFR inhibitor, >98% (HPLC)

IUPAC Name : N-(2-((2-(Dimethylamino)ethyl)(methyl)amino)-5-(4-(isopropylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)acrylamide

Price And Availability
Pack Size	Price in USD	Add To Shopping Cart	Availability	Shipping Status
5MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
10MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
25MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
50MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
100MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026

Applications : This is an orally bioavailable furanopyrimidine EGFR inhibitor engineered for high selectivity toward the L858R/T790M double‑mutant EGFR. Strategic replacement of the (S)-2‑phenylglycinol unit and incorporation of solubilizing groups into phenyl rings A and B yielded a lead compound with strong mutant‑selective cellular potency, showing an 8‑fold preference for H1975 (L858R/T790M) over A431 (WT EGFR). Western blot analysis confirms mutant‑EGFR target engagement. The compound demonstrates robust in vivo antitumor efficacy in BaF3‑mutant EGFR and H1975 xenografts (TGI = 74.9% and 97.5%) with 27% oral bioavailability. Its exceptionally selective kinome profile (S₁₀ = 0.017) supports advancement into detailed preclinical development as a promising double‑mutant EGFR inhibitor.

References : Li M-C. et al.: J. Med. Chem., 66(4), 2566-2588, 2023.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.