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CID5721353

Basic information Safety Supplier Related

CID5721353 Basic information

Product Name:
CID5721353
Synonyms:
  • CID5721353
  • CID5721353, BCL6 inhibitor
  • BCL6 inhibitor(CID5721353)
  • CID5721353 BDL6 inhribitor
  • CID-5721353;CID 5721353
  • 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
CAS:
301356-95-6
MF:
C15H9BrN2O6S2
MW:
457.28
Product Categories:
  • API
Mol File:
301356-95-6.mol
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CID5721353 Chemical Properties

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
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CID5721353 Usage And Synthesis

Description

CID-5721353 is an inhibitor of the transcriptional repressor B cell lymphoma 6 (Bcl-6; Ki = 147 μM). 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

CID5721353Supplier

Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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sales@meilune.com
Guangzhou Isun Pharmaceutical Co., Ltd
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020-39119399 18927568969
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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3008007409@qq.com
Tianjin Kailiqi Biotechnology Co., Ltd.
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15076683720
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klq@cw-bio.com