| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
The enzymatic activity of RNR is dose-dependently inhibited by TAS1553 (0.001-1 μM) [1]. With GI50 values ranging from 0.228 to 4.15 μM, TAS1553 (3 d) exhibits antiproliferative action against both solid and hematological human cancer cell lines [1]. In a dose- and time-dependent way, TAS1553 (1-10 μM; 0-2 hours; HCC38 and MV-4-11 cells) lowers the intracellular pool of dATP, a crucial metabolite for DNA replication [1]. In HCC38 and MV-4-11 cells, TAS1553 (0-10 μM; 0-24 hours) promotes apoptosis and replication stress in a dose- and time-dependent manner [1].
|
|---|---|
| ln Vivo |
RNR inhibitory effects have been observed in vivo for TAS1553 (25-200 mg/kg; oral; for 24 hours; female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice) [1]. In vivo anti-tumor activity has been demonstrated for TAS1553 (50-200 mg/kg; oral; daily for 15 d; female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice) [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: HCC38 and MV-4-11 Cell Tested Concentrations: 0, 0.1, 0.3, 1, 3 and 10 μM Incubation Duration: 0, 1, 2, 4, 8 and 24 hrs (hours) Experimental Results: Increased Ser345 , expression of Ser4, Ser8 and Thr21 phosphorylation. Increased levels of cleaved PARP and cleaved caspase-3. |
| Animal Protocol |
Animal/Disease Models: Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu (nude) mice [1]
Doses: 25, 50, 100 and 200 mg/kg Route of Administration: Oral; 200 mg/kg. 24 hour Experimental Results: diminished intracellular dATP pools and induced replicative stress and apoptosis. Animal/Disease Models: Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu (nude) mice [1] Doses: 50, 100 and 200 mg/kg Route of Administration: po (po (oral gavage)) one time/day for 15 days. Experimental Results: The tumor growth inhibition rates (T/C) of the treatment group/control group were 52.0 (50mg/kg), 45.0 (100mg/kg) and 29.4% (200mg/kg) respectively. |
| References |
[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.
|
| Molecular Formula |
C20H20CLFN4O5S
|
|---|---|
| Molecular Weight |
482.913005828857
|
| Exact Mass |
482.082
|
| CAS # |
2166023-31-8
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.1
|
| SMILES |
CC1=C(C(=C(C=C1)F)[C@@H](C)[C@@H](C2=NNC(=O)O2)NS(=O)(=O)C3=C(C=C(C=C3)Cl)C(=O)N)C
|
| InChi Key |
DUYRWEBTZNUILI-DIFFPNOSSA-N
|
| InChi Code |
InChI=1S/C20H20ClFN4O5S/c1-9-4-6-14(22)16(10(9)2)11(3)17(19-24-25-20(28)31-19)26-32(29,30)15-7-5-12(21)8-13(15)18(23)27/h4-8,11,17,26H,1-3H3,(H2,23,27)(H,25,28)/t11-,17+/m1/s1
|
| Chemical Name |
5-chloro-2-[[(1S,2R)-2-(6-fluoro-2,3-dimethylphenyl)-1-(2-oxo-3H-1,3,4-oxadiazol-5-yl)propyl]sulfamoyl]benzamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~207.08 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2071 mL | 1.0354 mL | 2.0708 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
