Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90mg/mL (186.4mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
TAS1553 2166023-31-8 Others TAS 1553 TAS-1553 inhibitor inhibit