2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. TAS-121

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.

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TAS-121 Chemical Structure

TAS-121 Chemical Structure

CAS No. : 1451370-01-6

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TAS-121 Related Antibodies

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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].

IC50 & Target[1]

EGFR L858R

1.7 nM (IC50)

EGFR (ex19del)

2.7 nM (IC50)

EGFR L858R/T790M

0.56 nM (IC50)

EGFR (ex19del/T790M)

1.1 nM (IC50)

EGFR (WT)

8.2 nM (IC50)

HER2

110 nM (IC50)

HER4

2.6 nM (IC50)

Molecular Weight

384.43

Formula

C22H20N6O
CAS No.
SMILES

NC1=C2C(C3=CC4=C(C=CC=C4)N=C3)=C5N(C[C@H](CC5)NC(C=C)=O)C2=NC=N1
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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.
Purity & Documentation
References
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TAS-121 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAS-1211451370-01-6TAS121TAS 121EGFRApoptosisEpidermal growth factor receptorErbB-1HER1OrallyEGFR-TKIL858REx19delL858R/T790MEx19del/T790MSW48NCI-H1975Inhibitorinhibitorinhibit

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