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CID5721353
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CID5721353图片
CAS NO:301356-95-6
包装:5mg, 10mg, 50mg
包装与价格:
包装价格(元)
10mM*1mL电议
5mg电议
10mg电议
50mg电议

产品名称
BCL6 inhibitor
产品介绍

生物活性

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.


化学数据

分子量457.28
分子式C15H9BrN2O6S2
CAS号301356-95-6
纯度100.0%
溶解性(25°C)DMSO: ≥ 40 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.1868 mL10.9342 mL21.8684 mL
5 mM0.4374 mL2.1868 mL4.3737 mL
10 mM0.2187 mL1.0934 mL2.1868 mL