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TAS0728

Cat. No. M10709

All AbMole products are for research use only, cannot be used for human consumption.

TAS0728  Structure
Size Price Availability Quantity
1mg USD 80  USD80 In stock
5mg USD 210  USD210 In stock
10mg USD 330  USD330 In stock
25mg USD 620  USD620 In stock
50mg USD 990  USD990 In stock
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Quality Control & Documentation
Biological Activity

TAS0728 is an effective, selective, oral, irreversible, covalently bound HER2 inhibitor covalently bound to the C805 site of HER2, inhibiting its activity.IC50 The value is 13 nM. TAS0728 to BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and HUMAN HER2 IC50 The values are 4.9, 8.5, 31, 65, 33, 25, 86, and 36 nM, respectively. TAS0728 simultaneously inhibits phosphorylation of HER2, HER3 and its downstream effector proteins. Has antitumor activity.

Chemical Information
Molecular Weight 504.58
Formula C26H32N8O3
CAS Number 2088323-16-2
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Sarina A Piha-Paul, et al. Invest New Drugs. A first-in-human phase I study of TAS0728, an oral covalent binding inhibitor of HER2, in patients with advanced solid tumors with HER2 or HER3 aberrations

[2] Hiroki Irie, et al. Cancer Sci. Acquired resistance to trastuzumab/pertuzumab or to T-DM1 in vivo can be overcome by HER2 kinase inhibition with TAS0728

[3] Hiroki Irie, et al. Mol Cancer Ther. TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models

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Keywords: TAS0728 supplier, EGFR/HER2, inhibitors, activators

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