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

TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors.

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TAS0728 Chemical Structure

TAS0728 Chemical Structure

CAS No. : 2088323-16-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 204 In-stock
Solution
10 mM * 1 mL in DMSO USD 204 In-stock
Solid
1 mg USD 90 In-stock
5 mg USD 184 In-stock
10 mg USD 288 In-stock
25 mg USD 544 In-stock
50 mg USD 880 In-stock
100 mg USD 1400 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

TAS0728 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors[1].

IC50 & Target[1]

HER4

8.5 nM (IC50)

HER2

13 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)

In Vitro

TAS0728 is a covalent-binding inhibitor of HER2 kinase and exhibits high selectivity for HER2 kinase. It also shows inhibitory activity against BMX, HER4, BLK, EGFR, JAK3, SLK, and LOK[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TAS0728 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HER2-amplified SK-BR-3/AU565/BT-474/NCI-N87/Calu-3 cells
Concentration:
Incubation Time:
Result: The GI50 values of TAS0728 were 5.0/5.1/3.6/1.6/6.9 nM relatively for HER2-amplified SK-BR-3/AU565/BT-474/NCI-N87/Calu-3 cells.
Inhibited the in vitro proliferation of five HER2-amplified cell lines.
Showed potent inhibitory activities against cancer cell lines with HER2 amplification.

Western Blot Analysis[1]

Cell Line: SK-BR-3 cells
Concentration: 30-300 nM
Incubation Time: 3 and 48 hours
Result: Showed sustained inhibition of HER2, HER3, AKT and ERK phosphorylation.
In Vivo

TAS0728 reveals the sustained and targeted inhibition of phosphorylation of HER2, HER3, AKT and ERK. TAS0728 also shows the ability of tumor regression and low toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male nude mice
Dosage: 7.5, 15, 30 and 60 mg/kg
Administration: Oral gavage; 7.5, 15, 30 and 60 mg/kg a day;14 days
Result: Rapidly eliminated within 24 hours.
Animal Model: Mice bearing NCI-N87 xenografts
Dosage: 60 mg/kg
Administration: Oral gavage; 60 mg/kg a day; 14 days
Result: Revealed sustained target inhibition of HER2, HER3, AKT and ERK.
Animal Model: Mice with NCI-N87 HER2–amplified human gastric cancer
Dosage: 7.5, 15, 30 and 60 mg/kg
Administration: Oral gavage; 7.5, 15, 30 and 60 mg/kg a day; 14 days
Result: Well tolerated in all mice.
Significant tumor regression was observed in mice treated with 60 mg/kg/day.
Animal Model: NCI-N87 peritoneal dissemination model
Dosage: 30 and 60 mg/kg
Administration: Oral gavage; 30and 60 mg/kg a day; 120 days
Result: No evident toxicity, including diarrhea and body weight loss in the long-term dosing of TAS0728.
Clinical Trial
Molecular Weight

504.58

Formula

C26H32N8O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=C2C(N([C@H]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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (247.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.15%

COA (264 KB) HNMR (216 KB) LCMS (122 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9818 mL 9.9092 mL 19.8185 mL 49.5462 mL
5 mM 0.3964 mL 1.9818 mL 3.9637 mL 9.9092 mL
10 mM 0.1982 mL 0.9909 mL 1.9818 mL 4.9546 mL
15 mM 0.1321 mL 0.6606 mL 1.3212 mL 3.3031 mL
20 mM 0.0991 mL 0.4955 mL 0.9909 mL 2.4773 mL
25 mM 0.0793 mL 0.3964 mL 0.7927 mL 1.9818 mL
30 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6515 mL
40 mM 0.0495 mL 0.2477 mL 0.4955 mL 1.2387 mL
50 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9909 mL
60 mM 0.0330 mL 0.1652 mL 0.3303 mL 0.8258 mL
80 mM 0.0248 mL 0.1239 mL 0.2477 mL 0.6193 mL
100 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4955 mL
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TAS0728 Related Classifications

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:

TAS07282088323-16-2TAS 0728TAS-0728EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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