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Theliatinib
$114 – $2,200
Products Details
Product Description
– Theliatinib (Xiliertinib) 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 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-104066
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C25H26N6O2
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
– 1353644-70-8
Molecular Weight
– 442.51
Compound Purity
– 99.77
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
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– DMSO : 1 mg/mL (ultrasonic;warming;adjust pH to 3 with HCl;heat to 60°C)|DMSO : 5 mg/mL (ultrasonic)
Target
– EGFR
Isoform
– EGFR/ErbB1/HER1
Pathway
– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
