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DI-87
🥰Excellent
Catalog No. T39550Cas No. 2107280-55-5
Alias TRE-515, TRE515, DI87
DI-87 (TRE-515) is a novel and orally available dCK (deoxycytidine kinase) inhibitor with good in vitro activity and low protein binding. DI-87 binds to dCK and prevents the phosphorylation of deoxycytidine by dCK, which reduces the production of dNTP and cell cycle arrest (especially in S phase). When combined with thymidine, DI-87 significantly inhibits tumor growth.
DI-87
🥰Excellent
Purity: 99.76%
Catalog No. T39550Alias TRE-515, TRE515, DI87Cas No. 2107280-55-5
DI-87 (TRE-515) is a novel and orally available dCK (deoxycytidine kinase) inhibitor with good in vitro activity and low protein binding. DI-87 binds to dCK and prevents the phosphorylation of deoxycytidine by dCK, which reduces the production of dNTP and cell cycle arrest (especially in S phase). When combined with thymidine, DI-87 significantly inhibits tumor growth.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $1,170 | In Stock | |
| 10 mg | $2,018 | In Stock |
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Purity:99.76%
ee:99%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | DI-87 (TRE-515) is a novel and orally available dCK (deoxycytidine kinase) inhibitor with good in vitro activity and low protein binding. DI-87 binds to dCK and prevents the phosphorylation of deoxycytidine by dCK, which reduces the production of dNTP and cell cycle arrest (especially in S phase). When combined with thymidine, DI-87 significantly inhibits tumor growth. |
| Targets&IC50 | DCK:10.2 nM (EC50) |
| In vitro | Methods: CEM cells were seeded at 1 × 10 3 cells/well in white opaque 384-well plates at 50 μl/well and treated as indicated. After incubation with increasing concentrations (2 nM-10 μM) of gemcitabine and 1 μM DI-87 for 72 h, 50 μl of CellTiter-Glo reagent (diluted 1:5 in dH2O) was added to each well, the plates were incubated at room temperature for 5 m, and luminescence was measured using a BioTek microplate luminometer. Results: The cytotoxic effect of gemcitabine requires dCK, and administration of DI-87 completely blocked cytotoxicity after gemcitabine treatment, demonstrating dCK inhibition by DI-87. [1] |
| In vivo | Methods: Female NSG mice bearing CEM tumors were treated with DI-87 (10, 25, or 50 mg/kg, orally) and DI-87 plasma and tumor concentrations were assessed. Results: Plasma DI-87 concentrations peaked between 1 and 3 hours; tumor concentrations were lower than plasma and had a later, more sustained peak at 3-9 hours. [1] |
| Alias | TRE-515, TRE515, DI87 |
| Molecular Weight | 502.65 |
| Formula | C23H30N6O3S2 |
| Cas No. | 2107280-55-5 |
| Smiles | COc1ccc(cc1OCCN1CCOCC1)-c1nc([C@@H](C)Sc2nc(N)cc(N)n2)c(C)s1 |
| Relative Density. | 1.37 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 120 mg/mL (238.73 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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