Theliatinib tartrate_product_DataBase

Bioactivity	Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases[1].
Invitro	Theliatinib tartrate 显着抑制 A431 细胞中的 EGFR 磷酸化，IC50 为 7 nM。Theliatinib 还抑制 A431、H292 和 FaDu 细胞存活，IC50 值分别为 80 nM、58 nM 和 354 nM[1]。
In Vivo	Theliatinib tartrate（2-15 mg/kg；口服；每天；21 天；NOD-SCID 小鼠；PDECX 1T0950 模型）导致小鼠模型中的肿瘤消退 75%，并且呈剂量依赖性[1]。
Name	Theliatinib tartrate
CAS	2413487-72-4
Formula	C29H32N6O8
Molar Mass	592.60
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]. Ren Y, et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget. 2017 Apr 19;8(31):50832-50844.

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