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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 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(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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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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