| Identification | Back Directory | [Name]
CID5721353 | [CAS]
301356-95-6 | [Synonyms]
CID5721353
BCL6 inhibitor
CID-5721353;CID 5721353
CID5721353, BCL6 inhibitor
BCL6 inhibitor(CID5721353)
CID5721353 BDL6 inhribitor
79-6 (CID5721353， BCL6 inhibitor)
CID 5721353;CID-5721353;CID 5721353
2-(5-(5-bromo-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)succinic acid
Butanedioic acid, 2-[5-(5-bromo-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinyl]- | [Molecular Formula]
C15H9BrN2O6S2 | [MDL Number]
MFCD31729277 | [MOL File]
301356-95-6.mol | [Molecular Weight]
457.28 |
| Chemical Properties | Back Directory | [density ]
2.06±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
3.02±0.23(Predicted) | [color ]
Light brown to brown |
| Hazard Information | Back Directory | [Description]
CID-5721353 is an inhibitor of the transcriptional repressor B cell lymphoma 6 (Bcl-6; Ki = 147 μM).1 It is selective for Bcl-6 over Kaiso, hypermethylated in cancer 1 (HIC1), and promyelocytic leukemia zinc finger (PLZF) at 50 μM. CID-5721353 is cytotoxic against Bcl-6-dependent SU-DLH-6, SU-DLH-4, Farage, OCI-LY7, OCI-LY1, and OCI-LY10 diffuse large B cell lymphoma (DLBCL) cells (GI50s = 0.024-0.936 mM) but not Bcl-6-independent Toledo or OCI-LY4 DLBCL cells (GI50 = >15 mM for both). It increases expression of the Bcl-6 target genes ATR, TP53, CD69, p21, and CD44 in SU-DLH-6 and SU-DHL-4 cells when used at a concentration of 50 μM. CID-5721353 (50 mg/kg) reduces tumor growth in OCI-LY7 and SU-DHL-6 mouse xenograft models. | [Uses]
CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM. | [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]. | [References]
[1] 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. DOI:10.1016/j.ccr.2009.12.050 |
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