Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selectiveEGFRinhibitor with aK_iof 0.05 nM and anIC₅₀of 3 nM. Theliatinib has anIC₅₀of 22 nM forEGFRT790M/L858R mutant. Theliatinib shows >50-fold selectivity forEGFRthan other kinases. Anti-tumor activity^[1].

Theliatinib significantly inhibits EGFR phosphorylation in A431 cells with an IC₅₀of 7 nM. Theliatinib also inhibits A431, H292 and FaDu cells survival with IC₅₀values of 80 nM, 58 nM and 354 nM, respectively^[1].

Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response^[1].

442.51

Solid

C₂₅H₂₆N₆O₂

1353644-70-8

西利替尼

Room temperature in continental US; may vary elsewhere.

DMSO : 5 mg/mL(11.30 mM;Need ultrasonic)

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