Theliatinib tartrate

Modify Date: 2024-04-08 10:13:46

Theliatinib tartrate structure	Common Name	Theliatinib tartrate
	CAS Number	2413487-72-4	Molecular Weight	592.60
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₉H₃₂N₆O₈	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Theliatinib tartrate

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].

Name	Theliatinib tartrate

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
In Vitro	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; 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].
References	[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.

Molecular Formula	C₂₉H₃₂N₆O₈
Molecular Weight	592.60

Theliatinib tartrate

Use of Theliatinib tartrate

Names

Theliatinib tartrate Biological Activity

Chemical & Physical Properties