1. Apoptosis
  2. Apoptosis
  3. DB2313

DB2313 is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects.

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DB2313 Chemical Structure

DB2313 Chemical Structure

CAS No. : 2170606-74-1

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Based on 1 publication(s) in Google Scholar

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Description

DB2313 is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects[1].

IC50 & Target

IC50: 14 nM (PU.1)[1]

In Vitro

DB2313 treatment leads to a profound decrease in the growth of PU.1 URE–/– acute myeloid leukemia (AML) cells (IC50 of 7.1 μM), while showing little effect on normal hematopoietic cells at similar concentrations. DB2313 treatment leads to a 3.5-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells. DB2313 also leads to a significant decrease in clonogenicity in the second and third rounds of plating and a complete disruption of clonogenic capacity in the fourth and higher rounds of plating[1].
In AML cells, DB2313 decreases PU.1 occupancy on E2f1, Junb, and Csf1r promoters[1].

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

In Vivo

DB2313 (17 mg/kg; i.p.; three times per week; for 3 weeks) treatment decreases leukemia progression and results in increased survival in mice[1].

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

Animal Model: NSG mice bearing sublethally irradiated (2.0 Gy) and injection with PU.1 URE–/– AML cells[1]
Dosage: 17 mg/kg
Administration: Intraperitoneal injection; three times per week; for 3 weeks
Result: Decreased tumor burden and resulted in increased survival.
Molecular Weight

708.83

Formula

C42H41FN8O2

CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

FC1=C(COC2=CC=C(C3=NC4=CC=C(C(NC(C)C)=N)C=C4N3)C=C2)C=CC=C1COC5=CC=C(C6=NC7=CC=C(C(NC(C)C)=N)C=C7N6)C=C5

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 : 100 mg/mL (141.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4108 mL 7.0539 mL 14.1078 mL
5 mM 0.2822 mL 1.4108 mL 2.8216 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: ≥ 3.33 mg/mL (4.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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: 3.33 mg/mL (4.70 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3.33 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 (33.3 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 5 mg/mL (7.05 mM); Suspended solution; Need ultrasonic

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 1.4108 mL 7.0539 mL 14.1078 mL 35.2694 mL
5 mM 0.2822 mL 1.4108 mL 2.8216 mL 7.0539 mL
10 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5269 mL
15 mM 0.0941 mL 0.4703 mL 0.9405 mL 2.3513 mL
20 mM 0.0705 mL 0.3527 mL 0.7054 mL 1.7635 mL
25 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4108 mL
30 mM 0.0470 mL 0.2351 mL 0.4703 mL 1.1756 mL
40 mM 0.0353 mL 0.1763 mL 0.3527 mL 0.8817 mL
50 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7054 mL
60 mM 0.0235 mL 0.1176 mL 0.2351 mL 0.5878 mL
80 mM 0.0176 mL 0.0882 mL 0.1763 mL 0.4409 mL
100 mM 0.0141 mL 0.0705 mL 0.1411 mL 0.3527 mL
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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.

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DB2313
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HY-124629
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