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Product 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]. Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Web ID
– HY-104066A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C29H32N6O8
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.
CAS Number
– 2413487-72-4
Molecular Weight
– 592.60
SMILES
– O=C(N1C[C@]2([H])N(C)CC[C@]2([H])C1)NC3=CC4=C(NC5=CC=CC(C#C)=C5)N=CN=C4C=C3OC.OC([C@H](O)[C@@H](O)C(O)=O)=O
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– EGFR
Pathway
– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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