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DI-87 

Cat. No.: HY-133141
Handling Instructions

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.

For research use only. We do not sell to patients.

DI-87 Chemical Structure

DI-87 Chemical Structure

CAS No. : 2107280-55-5

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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].

IC50 & 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.
Molecular Weight

502.65

Formula

C₂₃H₃₀N₆O₃S₂

CAS No.

2107280-55-5

SMILES

NC1=NC(S[[email protected]@H](C2=C(C)SC(C3=CC=C(OC)C(OCCN4CCOCC4)=C3)=N2)C)=NC(N)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

DI-87DI87DI 87OthersorallydeoxycytidinekinasedCKantitumorCCRF-CEMCEMInhibitorinhibitorinhibit

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DI-87
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