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TAS1553 is a potent, orally active protein–protein interaction (PPI) inhibitor with an IC50 values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research.

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TAS1553 Chemical Structure

TAS1553 Chemical Structure

CAS No. : 2166023-31-8

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Based on 1 publication(s) in Google Scholar

TAS1553 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

TAS1553 is a potent, orally active protein–protein interaction (PPI) inhibitor with an IC50 values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research[1].

In Vitro

TAS1553 (0.001-1 μM) inhibits the enzymatic activity of RNR in a dose-dependent manner[1].
TAS1553 (3 d) has anti-proliferative activity against both solid and hematological human cancer cell lines and the GI50 values ranged from 0.228 to 4.15 μM[1].
TAS1553 (1-10 μM; 0-2 h; HCC38 and MV-4-11 cells) reduces intracellular dATP pool in a dose- and time-dependent manner, which is a critical metabolite for DNA replication[1].
TAS1553 (0-10 μM; 0-24 h; HCC38 and MV-4-11 cells) induces the replication stress and apoptosis in a dose- and time-dependent manner[1].

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

TAS1553 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCC38 and MV-4-11 cells
Concentration: 0, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 0, 1, 2, 4, 8 and 24 hours
Result: Increased the expression of Ser345, Ser4, Ser8 and Thr21 phosphorylation. Increaed the levels cleaved PARP and cleaved caspase-3.
In Vivo

TAS1553 (25-200 mg/kg; p.o.; for 24 h; female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice) has RNR inhibition effect in vivo[1].
TAS1553 (50-200 mg/kg; p.o.; daily, for 15 d; female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice) has antitumor activity in vivo[1].

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

Animal Model: Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice[1]
Dosage: 25, 50, 100 and 200 mg/kg
Administration: Oral administration; for 24hours
Result: Reduces intracellular dATP pool and induces the replication stress and apoptosis.
Animal Model: Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice[1]
Dosage: 50, 100 and 200 mg/kg
Administration: Oral administration; daily, for 15 days
Result: Inhibited tumor growth in the treated group/control group (T/C) were 52.0 (50 mg/kg), 45.0 (100 mg/kg) and 29.4% (200 mg/kg), respectively.
Clinical Trial
Molecular Weight

482.91

Formula

C20H20ClFN4O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C1=CC(Cl)=CC=C1S(=O)(N[C@H](C(O2)=NNC2=O)[C@@H](C3=C(C)C(C)=CC=C3F)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (207.08 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 2.0708 mL 10.3539 mL 20.7078 mL
5 mM 0.4142 mL 2.0708 mL 4.1416 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.5 mg/mL (5.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.43%

SDS (252 KB)

COA (259 KB) HNMR (273 KB) LCMS (95 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0708 mL 10.3539 mL 20.7078 mL 51.7695 mL
5 mM 0.4142 mL 2.0708 mL 4.1416 mL 10.3539 mL
10 mM 0.2071 mL 1.0354 mL 2.0708 mL 5.1769 mL
15 mM 0.1381 mL 0.6903 mL 1.3805 mL 3.4513 mL
20 mM 0.1035 mL 0.5177 mL 1.0354 mL 2.5885 mL
25 mM 0.0828 mL 0.4142 mL 0.8283 mL 2.0708 mL
30 mM 0.0690 mL 0.3451 mL 0.6903 mL 1.7256 mL
40 mM 0.0518 mL 0.2588 mL 0.5177 mL 1.2942 mL
50 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0354 mL
60 mM 0.0345 mL 0.1726 mL 0.3451 mL 0.8628 mL
80 mM 0.0259 mL 0.1294 mL 0.2588 mL 0.6471 mL
100 mM 0.0207 mL 0.1035 mL 0.2071 mL 0.5177 mL
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TAS1553 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:

TAS15532166023-31-8TAS 1553TAS-1553OthersDNA replicationdATP poolapoptosisanticancerHCC38 cellMV-4-11 cellreplication stressInhibitorinhibitorinhibit

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