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CID5721353

CAS No. : 301356-95-6

MCE 站：CID5721353

产品活性：CID5721353 是一种 BCL6 抑制剂，IC₅₀ 为 212 μM，K_i值为 147 μM。

研究领域：Apoptosis

作用靶点：Bcl-2 Family  |  Apoptosis

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.

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.

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