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依喜替康甲磺酸鹽

NMR下載 COA and HPLC MSDS下載
names：
Exatecan Mesylate
CAS號：
169869-90-3
MDL Number： MFCD04113012
MF(分子式)： C25H26FN3O7S MW(分子量)： 531.55
EINECS: Reaxys Number:
Pubchem ID:6918249 Brand:BIOFOUNT

依沙替康甲磺酸鹽(169869-90-3,Exatecan Mesylate) 是一種有效的 DNA 拓撲異構(gòu)酶 I (topoisomerase I) 的抑制劑，IC50值是 2.2 μM (0.975 μg/mL)，可用于癌癥研究

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM002770-100mg	100mg	99%	￥ 0.00	￥ 0.00	2-3天	- +	￥ 0.00
YZM002770-10mg	10mg	99%	￥ 7980.00	￥ 7980.00	2-3天	- +	￥ 0.00
YZM002770-5mg	5mg	99%	￥ 4680.00	￥ 4680.00	2-3天	- +	￥ 0.00
YZM002770-1mg	1mg	99%	￥ 1580.00	￥ 1580.00	2-3天	- +	￥ 0.00

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中文別名	依喜替康甲磺酸鹽;依沙替康甲磺酸鹽(169869-90-3,Exatecan Mesylate);依喜替康甲磺酸鹽
英文別名	Exatecan Mesylate(169869-90-3);Exatecan mesilate;Exatecan (Mesylate);DX 8951f;DX-8951f
CAS號	169869-90-3
Inchi	InChI=1S/C24H22FN3O4.CH4O3S/c1-3-24(31)14-6-18-21-12(8-28(18)22(29)13(14)9-32-23(24)30)19-16(26)5-4-11-10(2)15(25)7-17(27-21)20(11)19;1-5(2,3)4/h6-7,16,31H,3-5,8-9,26H2,1-2H3;1H3,(H,2,3,4)/t16-,24-;/m0./s1
InchiKey	BICYDYDJHSBMFS-GRGFAMGGSA-N
分子式 Formula	C25H26FN3O7S
分子量 Molecular Weight	531.55
溶解度Solubility	生物體外In Vitro:DMSO溶解度8.33 mg/mL(15.67 mM;Need ultrasonic)H2O : 6 mg/mL(11.29 mM;Need ultrasonic and warming)
性狀	棕色到卡其色固體粉末
儲藏條件 Storage conditions	4°C，在氮氣下儲存

依沙替康甲磺酸鹽(169869-90-3,Exatecan Mesylate)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染

Exatecan Mesylate(169869-90-3) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tag:依沙替康甲磺酸鹽(169869-90-3,Exatecan Mesylate),依沙替康甲磺酸鹽試劑,依沙替康甲磺酸鹽的純度,依沙替康甲磺酸鹽的廠家,依沙替康甲磺酸鹽的價格,依沙替康甲磺酸鹽的作用,依沙替康甲磺酸鹽的外觀,依沙替康甲磺酸鹽的溶解度,依沙替康甲磺酸鹽的MSDS

產(chǎn)品說明	依喜替康甲磺酸鹽(169869-90-3,Exatecan Mesylate)是喜樹堿的半合成水溶性衍生物，具有抗腫瘤活性。
Introduction	Exatecan mesylate (169869-90-3,依沙替康甲磺酸鹽) is a semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity.
Application1	依沙替康甲磺酸鹽可通過穩(wěn)定拓撲異構(gòu)酶I與DNA之間的可裂解復(fù)合物并抑制DNA斷裂的連接來抑制拓撲異構(gòu)酶I的活性，從而抑制DNA復(fù)制并觸發(fā)凋亡性細胞死亡。
Application2	依沙替康甲磺酸鹽不需要酶促活化，并且比喜樹堿和其他喜樹堿類似物具有更高的效力。
Application3

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

Key role of topoisomerase I inhibitors in the treatment of recurrent and refractory epithelial ovarian carcinoma(Expert review of anticancer therapy,2008)

Relationship between drug release of DE-310, macromolecular prodrug of DX-8951f, and cathepsins activity in several tumors(Biological & pharmaceutical bulletin,2007)

Does consolidation with autologous stem cell transplantation improve the outcome of children with metastatic or relapsed Ewing sarcoma?(Pediatric blood & cancer,2007)

Exatecan in pretreated adult patients with advanced soft tissue sarcoma: results of a phase II--study of the EORTC Soft Tissue and Bone Sarcoma Group

Quantitative acid hydrolysis of DE-310, a macromolecular carrier system for the camptothecin analog DX-8951f(Journal of pharmaceutical and biomedical analysis,2007)

1. A phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for 5 days every 3 weeks to patients with advanced ovarian, tubal or peritoneal cancer resistant to platinum, taxane and topotecan
Claire F. Verschraegen, Andrzej P. Kudelka, Wei Hu. Cancer Chemother Pharmacol (2004) 53: 1–7
Exatecan mesylate (DX-8951f) is a synthetic derivative of camptothecin, a natural alkaloid extracted from the bark and leaves of the tree, Camptotheca acuminata. The activity of the drug is linked to its lactone form, which is in equilibrium with a carboxylate (open E ring) form. The equilibrium favors the carboxylate form at physiologic pH. The chemical structure of exatecan mesylate (DX-8951f) has been modi?ed to render the molecule water soluble by adding a ring structure between rings A (in position 9) and B (in position 7), and a ?uor in position 11. DX-8951f has shown both high in vitro potency against a series of 32 malignant cell lines and signi?cant topoisomerase I inhibition. The antiproliferative activity of exatecan mesylate (DX-8951f) in this system was 28 times greater than that of topotecan, and the antiproliferative activity of DX-8951f was about seven times greater than that of SN-38 (an active metabolite of irinotecan). Because of the demonstration of greater activity of DX-8951f than other camptothecin derivatives at equimolar concentrations in these pre- clinical studies, this phase II study was initiated.

2. DE-310, a macromolecular prodrug of the topoisomerase-I-inhibitor exatecan (DX-8951), in patients with operable solid tumors
Moritz N. Wente1 ,Jorg Kleeff, Markus W. Buchler. Investigational New Drugs 23: 339–347, 2005.
One of the recently introduced members of camptothecin analogs, exatecan mesylate (DX-8951f), is a synthetic water-soluble hexacyclic camptothecin analogue with broad anti-tumor activity. In pre-clinical studies, DX-8951 revealed highly potent inhibition of tumor cell growth in vitro and in vivo,evenin cells resistant to other members of the camptothecin family. In com- parison to other camptothecins, DX-8951 showed up to 20-fold higher topoisomerase-I inhibition and up to 30-fold more potent cell growth inhibition in vitro in various cancer cell lines.With its anti-tumor activity against irinotecan- and topotecan-resistant tumors, in phase II clinical DX-8951 demonstrated anti-tumor activity in several cancer types; phase III studies in pancreatic cancerare ongoing.

3. A phase II clinical and pharmacokinetic study of intravenous exatecan mesylate (DX-8951f) in patients with untreated metastatic gastric cancer
Jaffer A. Ajani, Chris Takimoto, Carlos R. Becerra. Investigational New Drugs 23: 479–484, 2005
Exatecan mesylate (DX-8951f; Daiichi Pharmaceutical Co., Ltd., Japan) is a synthetic camptothecin analogue (Figure 1) that is amore potent inhibitor of topoisomerase I than camptothecin, topotecan, and the active metabolite of irinotecan, SN-38. In preclinical studies, DX-8951f demonstrated broad antitumor activity compared with available camptothecin analogues. Cyclical dosing at lower doses demonstrated higher antitumor activity compared to single dose administration. Furthermore, the antitumor activity documented in phase I trials made DX-8951f an attractive compound for clinical development. We have completed a phase II trial designed to evaluate the activity and toxicity of exatecan mesylate (DX-8951f) in patients with previously untreated gastric carcinoma given as a thirty minute infusion daily for 5 days every 3 weeks. This schedule was selected from six phase I regimens because of the level of antitumor activity observed and its favorable toxicity pro?le.

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