1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. TAS0728

TAS0728 

Cat. No.: HY-111553 Purity: 99.53%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 389 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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)

Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (247.73 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9818 mL 9.9092 mL 19.8185 mL
5 mM 0.3964 mL 1.9818 mL 3.9637 mL
10 mM 0.1982 mL 0.9909 mL 1.9818 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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TAS0728
Cat. No.:
HY-111553
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