1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. CH-0793076

CH-0793076 (Synonyms: TP3076)

目录号: HY-107096
产品使用指南

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。

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CH-0793076 Chemical Structure

CH-0793076 Chemical Structure

CAS No. : 534605-78-2

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  • 生物活性

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  • 参考文献

生物活性

CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein)[1].

IC50 & Target[1]

Topoisomerase I

2.3 μM (IC50)

体外研究
(In Vitro)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

458.51

Formula

C26H26N4O4

CAS 号
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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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HY-107096
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