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DI-82
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Catalog No. T39114Cas No. 1638148-50-1
DI-82 is a highly potent inhibitor of deoxycytidine kinase (dCK), displaying impressive biochemical activity with an IC50 value of 27.8 nM and a K i value of 9.2 nM. Additionally, DI-82 exhibits significant antitumor effects.
DI-82
🥰Excellent
Catalog No. T39114Cas No. 1638148-50-1
DI-82 is a highly potent inhibitor of deoxycytidine kinase (dCK), displaying impressive biochemical activity with an IC50 value of 27.8 nM and a K i value of 9.2 nM. Additionally, DI-82 exhibits significant antitumor effects.
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Product Introduction
Bioactivity
Chemical Properties
| Description | DI-82 is a highly potent inhibitor of deoxycytidine kinase (dCK), displaying impressive biochemical activity with an IC50 value of 27.8 nM and a K i value of 9.2 nM. Additionally, DI-82 exhibits significant antitumor effects. |
| Targets&IC50 | DCK:27.8 nM (IC50app), DCK:9.2 nM (Kiapp) |
| In vitro | DI-82 (compound 12R) exhibits an IC50 value of 3.7 nM against acute lymphoblastic leukemia cells (CCRF-CEM)[1]. In liver microsomes, DI-82 demonstrates a NADPH-dependent intrinsic clearance (CLint) of 22.7 μL/min/mg and a half-life (T1/2) of 102 minutes at a concentration of 1 μM, indicating significant metabolic stability[1]. Additionally, at a concentration of 200 μM, DI-82 effectively inhibits the interaction between decitabine and human thymidylate synthase (TS), completely blocking the binding[2]. |
| Molecular Weight | 510.65 |
| Formula | C20H26N6O4S3 |
| Cas No. | 1638148-50-1 |
| Smiles | COc1ccc(cc1OCCNS(C)(=O)=O)-c1nc([C@@H](C)Sc2nc(N)cc(N)n2)c(C)s1 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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% Saline/PBS/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 μLSaline/PBS/ddH2O 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 μLSaline/PBS/ddH2O 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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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
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