(S)-10-Hydroxycamptothecin|19685-09-7|(10-羟基喜树碱; 10-HCPT; 10-Hydroxycamptothecin)-陌孚医药/Medlife

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(S)-10-Hydroxycamptothecin (Synonyms: 10-羟基喜树碱; 10-HCPT; 10-Hydroxycamptothecin)

目录号: PC10361 纯度: ≥98%

CAS No. :19685-09-7

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中文名称	(S)-10-Hydroxycamptothecin
中文别名	羟基喜树碱;(S)-10-羟基喜树碱;(20S)-10-羟基喜树碱;10-羟基喜树碱;(S)-4-乙基-4,9-二羟基-1H-吡喃并[3’,4’:6,7]吲嗪并[1,2-b]喹啉-3,14-(4H,12H)-二酮;10-S-羟基喜树碱;10-羟基喜树碱标准品;10-羟基喜树碱(RG);10-羟基喜树碱, 来源于红豆杉;10-羟基喜树碱植物提取物,标准品,对照品;阿尼西坦;羟喜树碱;神經胺[糖]酸;喜树碱;盐酸伊立替康三水合物杂质标准品;伊立替康相关物质A USP标准品;(S)-4-乙基-4,9-二羟基-1H-吡喃并[3',4':6,7]吲嗪并[1,2-b]喹啉-3,14-(4H,12H)-二酮;伊立替康相关物质A;喜树果提取物;10-羟喜树碱;1-羟基喜树碱;喜树碱10-羟基杂质;伊立替康USP RC A;10-羟基喜树碱(替康类)
英文名称	(S)-10-Hydroxycamptothecin
英文别名	(S)-4-Ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione;Hydroxy Camptothecine;SN38;CAMPTOTHECIN, 10-HYDROXY-;CAMPTOTHECIN, 10-HYDROXY-, CAMPTOTHECA ACUMINATA;HCPT;HYDROXYCAMPTOTHECIN;HYDROXYCAMPTOTHECIN, 10-;(+/-)-4-ethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione;10Hydroxy camptothecin;7-Ethy Hydroxycamptothecin;10-HYDROXYCAMPTOTHECIN;(20S)-7-ETHYL-10-HYDROXYCAMPTOTHECIN;(S)-10-Hydroxycamptothecin;(S)-10-hydroxy-Camptothecin;Camptothecine;Ecdysterone;Hydrocamptothecine;HYDROXYCAMPTOTHECIN, 10-(RG);10-HCPT;10-Hydroxycamptochecin;10-hydroxycamptothecine;10-hydroxy-CPT;10-OH-camptothecin;Camptothecin,hydroxy;Irinotecan Related Compound A;(S)-4-Ethyl-4,9-dihydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione;(4S)-4-Ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione;NSC 107124;[ "" ];Ampule;hydroxy-camptotheci;Irinotecan USP RC A;10-HYDROCAMPTOTHECIN;Hydroxycamptothecine;Camptothecin, hydroxy-;10-Hydroxy camptothecin;10-Hydroxy-Camptothecin;Camptothecine, 10-hydroxy-;NSC;(+)-(S)-10-Hydroxycamptothecin;(20S)-10-Hydroxycamptothecin;9Z01632KRV;Camptothecin, 10-hydroxy;UNII:9Z01632KRV;10-HCPT;10-Hydroxycamptothecin;10-Hydroxy Camptothecin-d5;10-Hydroxycamp-totecin;10-hydroxycamptothecin98%;10-HYDROXYCAMTOTHECIN;1H-Pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H,12H)-dione, 4-ethyl-4,9-dihydroxy-, hydrate, (S)-;1H-Pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H,12H)-dione-,4-ethyl-4,9-dihydroxy-, (S)- (9CI);BR-33939;BSPBio_003281;Camptothecine, 10-hydroxy- (8CI);Hydroxycamptothecin-10;NCGC00095986-01;SPECTRUM1504123;Spectrum5_000549;STOCK1N-67892;TL8001609;UNII-9Z01632KRV
Cas No.	19685-09-7
分子式	C₂₀H₁₆N₂O₅
分子量	364.35
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.

性状

Solid

IC50 & Target[1][2]

Topoisomerase I

体外研究(In Vitro)

(S)-10-Hydroxycamptothecin (5-20 μg/L; 6 days; Hep G2 cells) treatment results in the cell cycle arrest at G2/M phase.
(S)-10-Hydroxycamptothecin induces differentiation, down-regulates nuclear antigen (PCNA) and up-regulates wild-type protein p53 in Hep G2 cells.
(S)-10-Hydroxycamptothecin inhibits L1210 leukemia cells with an IC₅₀ of 1.15 μM.

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

Cell Cycle Analysis

Cell Line:	Hep G2 cells
Concentration:	5 μg/L, 10 μg/L, 20 μg/L
Incubation Time:	6 days
Result:	Hep G2 cells were mainly arrested at G2/M phase.

体内研究(In Vivo)

(S)-10-Hydroxycamptothecin (10-Hydroxycamptothecin) against L1210 leukemia in mice is tested. At the optimal dose (15 mg/kg), (S)-10-Hydroxycamptothecin has a 71% increase in life span (ILS).

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

结构分类

来源

参考文献

[1]. Min Liu, et al. Intracellular delivery of 10-hydroxycamptothecin with targeted nanostructured lipid carriers against multidrug resistance . Journal of Drug Targeting.

[2]. Min Liu, et al. Intracellular delivery of 10-hydroxycamptothecin with targeted nanostructured lipid carriers against multidrug resistance. J Drug Target, Early Online: 1–8

[3]. Yu P, et al. Synthesis and preliminary anticancer evaluation of 10-hydroxycamptothecin analogs. Biol Pharm Bull. 2012;35(8):1295-9. [Information]

[4]. Zhang XW, et al. Differentiation-inducing action of 10-hydroxycamptothecin on human hepatoma Hep G2 cells. Acta Pharmacol Sin. 2000 Apr;21(4):364-8. [Information]

[5]. Zhang XW, et al. Differential regulation of P53, c-Myc, Bcl-2, Bax and AFP protein expression, and caspase activity during 10-hydroxycamptothecin-induced apoptosis in Hep G2 cells. Anticancer Drugs. 2000 Oct;11(9):747-56. [Information]

[6]. Liu M, et al. Intracellular delivery of 10-hydroxycamptothecin with targeted nanostructured lipid carriers against multidrug resistance. J Drug Target. 2016;24(5):433-40. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (137.23 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7446 mL	13.7231 mL	27.4461 mL
5 mM	0.5489 mL	2.7446 mL	5.4892 mL
10 mM	0.2745 mL	1.3723 mL	2.7446 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (6.86 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.86 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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