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CH-0793076 (Synonyms: 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。
CH-0793076 Chemical Structure
CAS No. : 534605-78-2
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CH-0793076 的其他形式现货产品:
| 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]. |
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| IC50 & Target[1] |
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| 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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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| 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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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| 分子量 |
458.51 |
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| Formula |
C26H26N4O4 |
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| CAS 号 |
534605-78-2 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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| 参考文献 |
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