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

TAS0728 

Cat. No.: HY-111553
Handling Instructions

TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity.

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

TAS0728 Chemical Structure

TAS0728 Chemical Structure

CAS No. : 2088323-16-2

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity[1].

IC50 & Target[1]

HER4

8.5 nM (IC50)

HER2

13 nM (IC50)

Human HER2

36 nM (IC50)

EGFR

65 nM (IC50)

BMX

4.9 nM (IC50)

BLK

31 nM (IC50)

JAK3

33 nM (IC50)

SLK

25 nM (IC50)

LOK

86 nM (IC50)

References
Molecular Weight

504.58

Formula

C₂₆H₃₂N₈O₃

CAS No.

2088323-16-2

SMILES

NC1=C2C(N([[email protected]]3CN(C(C=C)=O)CCC3)N=C2C(NC4=CC=C(CC(N(C)C)=O)C(C)=C4C)=O)=NC=N1

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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TAS0728
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HY-111553
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TAS0728

Cat. No.: HY-111553