TP3011(Synonyms: CH0793011)

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TP3011 (Synonyms: CH0793011)

TP3011 (CH0793011) 是 CH-0793076 的活性代谢产物 (metabolite)，是与 SN38 等价的有效拓扑异构酶 I (topoisomerase I) 抑制剂。TP3011 在 IC50 亚纳摩尔范围内可抵抗癌细胞系的生长。

TP3011(Synonyms: CH0793011)

TP3011 Chemical Structure

CAS No. : 534605-74-8

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生物活性

TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38[1]. TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro[2].

IC50 & Target[1]

Topoisomerase I

 

体外研究
(In Vitro)

TP3011 (0-100 nM; 72 hours) (compound 6c) inhibits cell proliferative activities against various human cancer cell lines, producing 50% inhibition (IC50) of cell growth of 0.85 nM; 8.5 nM; and 8.2 nM in HCT116, QG56, and NCI-H460 (NSCLC) cells, respectively[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: HCT116, QG56, and NCI-H460 (NSCLC) cells
Concentration: 0-100 nM
Incubation Time: 72 hours
Result: Was against human cancer cell lines, such as CRC and NSCLC cell lines.

分子量

474.51

Formula

C26H26N4O5
CAS 号

534605-74-8
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.
参考文献

  • [1]. Anthoney DA, et al. Phase I study of TP300 in patients with advanced solid tumors with pharmacokinetic, pharmacogenetic and pharmacodynamic analyses.BMC Cancer. 2012 Nov 21;12:536.

    [2]. Niizuma S, et al. Synthesis of new camptothecin analogs with improved antitumor activities.Bioorg Med Chem Lett. 2009 Apr 1;19(7):2018-21.

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