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TAS-121

CAT: 0804-HY-164392Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-164392Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI) . TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM) . TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models[1].
CAS Number
1451370-01-6
UNSPSC
12352005
Target
Apoptosis; EGFR
Type
Reference compound
Related Pathways
Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/tas-121.html
Smiles
NC1=C2C(C3=CC4=C(C=CC=C4)N=C3)=C5N(C[C@H](CC5)NC(C=C)=O)C2=NC=N1
Molecular Formula
C22H20N6O
Molecular Weight
384.43
References & Citations
[1]Kimihiro Ito, et al. TAS-121, A Selective Mutant EGFR Inhibitor, Shows Activity Against Tumors Expressing Various EGFR Mutations Including T790M and Uncommon Mutations G719X. Mol Cancer Ther. 2019 May;18 (5) :920-928.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EGFR/ErbB1/HER1; ErbB2/HER2; ErbB4/HER4

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