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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.

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DI-87 Chemical Structure

DI-87 Chemical Structure

CAS No. : 2107280-55-5

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5 mg USD 550 In-stock
10 mg USD 880 In-stock
25 mg USD 1760 In-stock
50 mg USD 3000 In-stock
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Based on 1 publication(s) in Google Scholar

DI-87 Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DI-87 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NC1=NC(S[C@@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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 145 mg/mL (288.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9895 mL 9.9473 mL 19.8946 mL
5 mM 0.3979 mL 1.9895 mL 3.9789 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.97 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9895 mL 9.9473 mL 19.8946 mL 49.7364 mL
5 mM 0.3979 mL 1.9895 mL 3.9789 mL 9.9473 mL
10 mM 0.1989 mL 0.9947 mL 1.9895 mL 4.9736 mL
15 mM 0.1326 mL 0.6632 mL 1.3263 mL 3.3158 mL
20 mM 0.0995 mL 0.4974 mL 0.9947 mL 2.4868 mL
25 mM 0.0796 mL 0.3979 mL 0.7958 mL 1.9895 mL
30 mM 0.0663 mL 0.3316 mL 0.6632 mL 1.6579 mL
40 mM 0.0497 mL 0.2487 mL 0.4974 mL 1.2434 mL
50 mM 0.0398 mL 0.1989 mL 0.3979 mL 0.9947 mL
60 mM 0.0332 mL 0.1658 mL 0.3316 mL 0.8289 mL
80 mM 0.0249 mL 0.1243 mL 0.2487 mL 0.6217 mL
100 mM 0.0199 mL 0.0995 mL 0.1989 mL 0.4974 mL
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DI-87 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DI-872107280-55-5DI87DI 87OthersorallydeoxycytidinekinasedCKantitumorCCRF-CEMCEMInhibitorinhibitorinhibit

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