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TAS0728

Cat. No. M10709
TAS0728  Structure
Size Price Availability Quantity
5mg USD 360  USD360 In stock
25mg USD 1050  USD1050 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 504.58
Formula C26H32N8O3
CAS Number 2088323-16-2
Purity >99%
Solubility DMSO ≥ 100 mg/mL
Storage at -20°C
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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