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CID5721353

Cat. No. M9248
CID5721353 Structure
Synonym:

BCL6 Inhibitor

Size Price Availability Quantity
10mM*1mL In DMSO USD 97 In stock
5mg USD 90 In stock
10mg USD 150 In stock
50mg USD 487 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CID5721353 specifically inhibits BCL6 repressor activity. CID5721353 disrupts BCL6 transcriptional complexes and reactivates BCL6 target genes. CID5721353 can specifically kill primary human DLBCL cells. 79% BCL6-positive cases display greater than 25% loss of viability in response to CID5721353 at 125 or 250 μM. 

In vivo, 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 457.28
Formula C15H9BrN2O6S2
CAS Number 301356-95-6
Purity >98%
Solubility DMSO: ≥ 40 mg/mL
Storage at -20°C
References

A small-molecule inhibitor of BCL6 kills DLBCL cells in vitro and in vivo.
Cerchietti LC, et al. Cancer Cell. 2010 Apr 13;17(4):400-11. PMID: 20385364.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CID5721353, BCL6 Inhibitor supplier, inhibitors

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