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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
301356-95-6
- 规格:
10 mM * 1 mL/2 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥905.0 |
|---|---|---|---|
| 规格: | 2 mg | 产品价格: | ¥500.0 |
| 规格: | 5 mg | 产品价格: | ¥900.0 |
| 规格: | 10 mg | 产品价格: | ¥1500.0 |
| 规格: | 25 mg | 产品价格: | ¥2900.0 |
| 规格: | 50 mg | 产品价格: | ¥4900.0 |
| 规格: | 100 mg | 产品价格: | ¥8400.0 |
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CID5721353
CAS No. : 301356-95-6
MCE 国际站:CID5721353
产品活性:CID5721353 是一种 BCL6 抑制剂,IC50 为 212 μM,Ki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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