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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Description

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)

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].

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].

Molecular Weight

458.51

Formula

C₂₆H₂₆N₄O₄

CAS No.

534605-78-2

SMILES

O=C1[C@](O)(CC)C(C=C23)=C(CO1)C(N2CC(C3=N4)=C5N(CCCCC)C=NC6=C5C4=CC=C6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

CH-0793076TP3076CH0793076CH 0793076TP 3076TP-3076Topoisomerasebreastcancerresistancemetaboliteantiproliferativeanti-cancertoxicitycolorectalInhibitorinhibitorinhibit

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产品名称:
CH-0793076
目录号:
HY-107096
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