1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Theliatinib

Theliatinib (Synonyms: HMPL-309)

Cat. No.: HY-104066
Handling Instructions

Theliatinib (HMPL-309) is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.

For research use only. We do not sell to patients.

Theliatinib Chemical Structure

Theliatinib Chemical Structure

CAS No. : 1353644-70-8

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Description

Theliatinib (HMPL-309) is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively[1].

IC50 & Target

IC50: 3 nM (EGFR), 22 nM (EGFR T790M/L858R)[1]
Ki: 0.05 nM (EGFR)[1]

Molecular Weight

442.51

Formula

C₂₅H₂₆N₆O₂

CAS No.

1353644-70-8

SMILES

O=C(N1C[[email protected]]2([H])N(C)CC[[email protected]]2([H])C1)NC3=CC4=C(NC5=CC=CC(C#C)=C5)N=CN=C4C=C3OC

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TheliatinibHMPL-309HMPL309HMPL 309EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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