2. Apoptosis
  3. Bcl-2 Family Apoptosis
  4. CID5721353

CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM.

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CID5721353 Chemical Structure

CID5721353 Chemical Structure

CAS No. : 301356-95-6

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Based on 1 publication(s) in Google Scholar

CID5721353 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM.

IC50 & Target

IC50: 212 μM (BCL6)[1]
Ki: 147 μM(BCL6)[1]
In Vitro

BCL6 is a member of the BTB/POZ family of transcription factors. CID5721353 (Compound 79-6) specifically inhibits BCL6 repressor activity. CID5721353 disrupts BCL6 transcriptional complexes and reactivates BCL6 target genes. CID5721353 can specifically kill primary human DLBCL cells. Fifteen of 19 BCL6-positive cases (79%) display greater than 25% loss of viability in response to CID5721353 at 125 or 250 μM[1].

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

CID5721353 Related Antibodies
In Vivo

In order to test whether CID5721353 (Compound 79-6) can perform as an anti-lymphoma therapeutic agent in vivo, whether it can penetrate tumors after parenteral administration through a distal site is determined. For this purpose 107OCI-Ly7 cells are injected into the right flank of 10 SCID mice and allowed to form tumors. Once tumors reach ~1.5 grams, animals are injected IP with a single dose of 50 mg/kg of CID5721353 in 10% DMSO or vehicle (10% DMSO) and sacrificed at 0.5, 1, 1.5, 3, 6, 12 and 24 hours after CID5721353 administration. Blood and tumors are harvested. Quantitative HPLC/MS analysis of the serum shows that CID5721353 levels peak (to 55 μg/mL, which is equivalent to a 122 μM concentration) one hour after the IP injection. CID5721353 also reaches its highest peak (24.5 ng/mg) at the 1-hour time point in the tumors, and after a sharp decline in levels, decreases gradually over 24 hours[1].

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

457.28

Formula

C15H9BrN2O6S2
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

O=C(O)C(N(C/1=O)C(SC1=C2C(NC3=C\2C=C(Br)C=C3)=O)=S)CC(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (109.34 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 2.1868 mL 10.9342 mL 21.8684 mL
5 mM 0.4374 mL 2.1868 mL 4.3737 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
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

=
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 (5.47 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 (5.47 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 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
Cell Assay
[1]

Cell number and viability are determined by an EB/AO-based method and cells are cultivated in medium containing 80% RPMI and 20% human serum supplemented with antibiotics, L-glutamine and HEPES for 48 h. Pimary human diffuse large B cell lymphoma (DLBCL) cells are exposed to 125 and 250 μM of CID5721353 or control (DMSO) in triplicates. After 48 h of exposure viability is determined by using an ATP-based luminescent method and EB/AO. Specimens with 20% or higher loss of viability in the controls are discarded[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Six to eight-week old male SCID mice are subcutaneously injected in the left flank with low-passage 107 human OCI-Ly7 cells. When tumors reach 1500 mm3 the mice are IP injected with 50 mg/kg of CID5721353 in DMSO (n=8) or DMSO (control, n=2). Blood and tumors are harvested at different time points after injection (30 min, 1 h, 1.5 h, 3 h, 6 h, 12 h and 24 h)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1868 mL 10.9342 mL 21.8684 mL 54.6711 mL
5 mM 0.4374 mL 2.1868 mL 4.3737 mL 10.9342 mL
10 mM 0.2187 mL 1.0934 mL 2.1868 mL 5.4671 mL
15 mM 0.1458 mL 0.7289 mL 1.4579 mL 3.6447 mL
20 mM 0.1093 mL 0.5467 mL 1.0934 mL 2.7336 mL
25 mM 0.0875 mL 0.4374 mL 0.8747 mL 2.1868 mL
30 mM 0.0729 mL 0.3645 mL 0.7289 mL 1.8224 mL
40 mM 0.0547 mL 0.2734 mL 0.5467 mL 1.3668 mL
50 mM 0.0437 mL 0.2187 mL 0.4374 mL 1.0934 mL
60 mM 0.0364 mL 0.1822 mL 0.3645 mL 0.9112 mL
80 mM 0.0273 mL 0.1367 mL 0.2734 mL 0.6834 mL
100 mM 0.0219 mL 0.1093 mL 0.2187 mL 0.5467 mL
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CID5721353 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:

CID5721353301356-95-6CID 5721353CID-5721353Bcl-2 FamilyApoptosisInhibitorinhibitorinhibit

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