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TAS1553

Catalog No. T60217   CAS 2166023-31-8

TAS1553 is a highly effective, orally bioavailable protein-protein interaction (PPI) inhibitor with an IC50 value of 0.0396 μM. It effectively hinders DNA replication and diminishes the intracellular dATP pool. Moreover, TAS1553 induces apoptosis, making it a valuable compound in cancer research [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
TAS1553 Chemical Structure
TAS1553, CAS 2166023-31-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 98.00
2 mg In stock $ 145.00
5 mg In stock $ 247.00
10 mg In stock $ 372.00
25 mg In stock $ 629.00
50 mg In stock $ 896.00
100 mg In stock $ 1,220.00
1 mL * 10 mM (in DMSO) In stock $ 263.00
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Purity: 97.03%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TAS1553 is a highly effective, orally bioavailable protein-protein interaction (PPI) inhibitor with an IC50 value of 0.0396 μM. It effectively hinders DNA replication and diminishes the intracellular dATP pool. Moreover, TAS1553 induces apoptosis, making it a valuable compound in cancer research [1].
In vitro TAS1553 (0.001-1 μM) dose-dependently inhibits the enzymatic activity of RNR [1]. TAS1553 (3 d) has anti-proliferative activity against both solid and hematological human cancer cell lines and the GI 50 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]. 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) shows RNR inhibitory 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]. 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.
Molecular Weight 482.91
Formula C20H20ClFN4O5S
CAS No. 2166023-31-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90mg/mL (186.4mM), sonification is recommended.

TargetMolReferences and Literature

1. Ueno H, et, al. TAS1553, a small molecule subunit interaction inhibitor of ribonucleotide reductase, exhibits antitumor activity by causing DNA replication stress. Commun Biol. 2022 Jun 9;5(1):571.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Compound Library PPI Inhibitor Library Clinical Compound Library Drug Repurposing Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

TAS1553 2166023-31-8 Others TAS 1553 TAS-1553 inhibitor inhibit

 

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