2107280-55-5
2107280-55-5 structure
- Name: DI-87
- Chemical Name: DI-87
- CAS Number: 2107280-55-5
- Molecular Formula: C23H30N6O3S2
- Molecular Weight: 502.65
- Catalog: Signaling Pathways Others Others
- Create Date: 2020-08-11 15:49:09
- Modify Date: 2024-01-27 19:30:15
-
DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK[1].
| Name | DI-87 |
|---|
| Description | DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK[1]. |
|---|---|
| Related Catalog | |
| Target |
EC50: 10.2 nM (dCK)[1] |
| In Vitro | (S)-DI-87 exhibits a much higher IC50 value (IC50=468 nM) relative to DI-87 ((R)-DI-8) (IC50=3.15 nM) in CEM T-ALL cells for inhibition of dCK activity[1]. DI-87 (1 µM; for 72 hours) rescues human cell line CCRF-CEM (CEM) cells from the anti-proliferative effects of gemcitabine, a dCK-dependent nucleoside analog prodrug, with an EC50 of 10.2 nM[1]. |
| In Vivo | DI-87 (5-25 mg/kg; oral gavage) exhibits full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours with 25 mg/kg dose[1]. DI-87 (10-50 mg/kg; oral) has plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours[1]. DI-87 (10 mg/kg/day or 25 mg/kg/twice a day; oral; for 16-18 days) with thymidine (2 g/kg; ip; twice a day) results in reduced tumor growth in male NSG mice implanted with CEM tumors[1]. Animal Model: 8-12 week-old male or female NSG mice with CEM tumor xenografts[1] Dosage: 5, 10, 25 mg/kg Administration: Oral gavage Result: The 25 mg/kg dose exhibited full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours. The 10 mg/kg dose resulted in full inhibition with recovery initiating at the 12 hours time point. The 5 mg/kg dose resulted in minimal dCK inhibition with rapid recovery. Animal Model: Female NSG mice with CEM tumors[1] Dosage: 10, 25, or 50 mg/kg Administration: Oral Result: Had plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours. Had tumor concentrations lower than plasma and had a later, more sustained peak at 3-9 hours. |
| References |
| Molecular Formula | C23H30N6O3S2 |
|---|---|
| Molecular Weight | 502.65 |