CID5721353

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CID5721353
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Cat #: V4119 CAS #: 301356-95-6 Purity ≥ 98%

Description: CID5721353 (also known as BCL6 Inhibitor and 79-6) is a novel and potent inhibitor of BCL6 (B-Cell Lymphoma 6) with an IC50 value of 212 μM (equivalent to a Ki of 147 μM).

References: Cerchietti LC, et al. A small-molecule inhibitor of BCL6 kills DLBCL cells in vitro and in vivo. Cancer Cell. 2010 Apr 13;17(4):400-11.

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Molecular Weight (MW)457.27
Molecular FormulaC15H9BrN2O6S2
CAS No.301356-95-6
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: ≥ 90mg/mLr
Water: N/Ar
Ethanol: N/A
SMILES CodeO=C(O)C(N(C/1=O)C(SC1=C2C(NC3=C/2C=C(Br)C=C3)=O)=S)CC(O)=O
SynonymsBCL6 Inhibitor; 79-6; CID5721353; CID-5721353; CID 5721353
ProtocolIn VitroBCL6 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.
In VivoIn 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.1869 mL10.9345 mL21.8689 mL43.7378 mL
5mM0.4374 mL2.1869 mL4.3738 mL8.7476 mL
10mM0.2187 mL1.0934 mL2.1869 mL4.3738 mL
20mM0.1093 mL0.5467 mL1.0934 mL2.1869 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
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=
Concentration(final)
C2
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Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.