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CH-0793076
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。
CH-0793076图片
CAS NO:534605-78-2

TP3076
CH-0793076 (TP3076),喜树碱的六环类似物,是TP300 的活性药物和主要代谢物。CH-0793076 抑制 DNA 拓扑异构酶I (DNA topoisomerase I),IC50为 2.3 μM。CH-0793076 对表达 BCRP (乳腺癌耐药蛋白) 的细胞也有活性。
生物活性

CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibitsDNAtopoisomeraseIwith anIC50of 2.3 μM. CH-0793076 is efficacious against cells expressingBCRP(breastcancerresistance protein)[1].

IC50& Target[1]

Topoisomerase I

2.3 μM (IC50)

体外研究
(In Vitro)

CH0793076 (TP3076) (6 days at 37℃) shows antiproliferative activity against PC-6/BCRP and PC-6/pRC cells, with IC50s of 0.35 and 0.18 nM, respectively[1].

体内研究
(In Vivo)

TP300 (1-100 mg/kg; bolus intravenous injection once per week for 3 weeks, for a total of three doses), a water-soluble prodrug of CH0793076, shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP (WiDr, HT-29, NCI-H460 and AsPC-1, HCT116, COLO 201, HCT-15, Calu-6 and NCI-N87)[1].

分子量

458.51

Formula

C26H26N4O4

CAS 号

534605-78-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

 
 
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