DRF-1042|200619-13-2|-陌孚医药/Medlife

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DRF-1042

目录号: PL02752 纯度: ≥98%

CAS No. :200619-13-2

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中文名称	DRF-1042
中文别名	(4S)-4-乙基-4-羟基-12-(2-羟基乙氧基)-1H-吡喃并[3',4':6,7]吲哚嗪并[1,2-B]喹啉-3,14(4H,12H)-二酮
英文名称	DRF-1042
英文别名	DRF-1042;DRF-1042;DRF 1042
Cas No.	200619-13-2
分子式	C₂₂H₂₀N₂O₆
分子量	408.40
包装储存	-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情	DRF-1042 是一种具有口服活性的喜树碱类似物，具有抑制 DNA 拓扑异构酶 I (DNA topoisomerase I) 的作用。DRF-1042 对一组人癌细胞株，包括多药耐药 (MDR)表型，显示出良好的抗癌活性。
生物活性	DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
性状	Solid
IC50 & Target[1][2]	DNA topoisomerase I
体外研究(In Vitro)	DRF-1042 demonstrates superior lactone stability and good in vitro anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	In clonogenic assay against murine, canine and human bone marrow cells, DRF-1042 treatment shows less mylosupression that supports the possibility of protracted dose schedule in both experimental and clinical studies. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献	[1]. Chatterjee A, et al. Safety, tolerability, and pharmacokinetics of a capsule formulation of DRF-1042, a novelcamptothecin analog, in refractory cancer patients in a bridging phase I study. J Clin Pharmacol. 2005 Apr;45(4):453-60. [2]. Sriram Rajagopal, et al. Preclinical evaluation of the anticancer activity of DRF-1042, a novel camptothecin analog targeting Topoisomerase-I. Published April 2004.

溶解度数据	In Vitro: DMSO : 50 mg/mL (122.43 mM; Need ultrasonic)配制储备液

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