TX1-85-1
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling[1].
Product Specifications
CAS Number
[1603845-32-4]
UNSPSC
12352005
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/tx1-85-1.html
Purity
99.65
Solubility
DMSO : 3.85 mg/mL (ultrasonic)
Smiles
CC(N1CCN(C2CCC(N3N=C(C4=CC(NC(C=C)=O)=C(OC5=CC=CC=C5)C=C4)C6=C3N=CN=C6N)CC2)CC1)=O
Molecular Formula
C32H36N8O3
Molecular Weight
580.68
References & Citations
[1]Xie T, et al. Pharmacological targeting of the pseudokinase Her3. Nat Chem Biol. 2014 Dec;10 (12) :1006-12.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ErbB3/HER3
Available Sizes
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