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鹽酸吉西他濱是一種DNA合成抑制劑，其IC50值為240.4±29.0微米(CCRF-CEM/dCK/細(xì)胞)、14.7±2.8納米(TC-1細(xì)胞)、36.7±5.1微米(TC-1-GR細(xì)胞)和50納米(PANC1細(xì)胞)[1]。 DNA合成是DNA分子的自然或人工創(chuàng)造，可以定義為DNA復(fù)制、聚合酶鏈?zhǔn)椒磻?yīng)和基因合成。據(jù)報道，DNA合成過程在多種癌癥中起著重要作用，許多藥物已被制成針對這一過程來抑制腫瘤生長或轉(zhuǎn)移[2] [3]。

鹽酸吉西他濱是一種DNA合成抑制劑。當(dāng)用胰腺癌細(xì)胞系COLO 357和L3.6pl進行測試時，繼染料木黃酮(其使細(xì)胞對鹽酸吉西他濱敏感)之后的鹽酸吉西他濱治療顯著抑制了細(xì)胞生長并增加了細(xì)胞凋亡[4]。在MIA PaCa-2細(xì)胞中，鹽酸吉西他濱通過抑制dDNA的活性對細(xì)胞表現(xiàn)出顯著的細(xì)胞毒性，IC50值為49.7±17.7nM[1]。 在原位植入COLO 357細(xì)胞的SCID小鼠中，與對照組相比，經(jīng)染料木黃酮和吉西他濱治療的小鼠顯著降低(75%，P < 0.01)腫瘤生長和體重[4]。

產(chǎn)品性質(zhì)：

Cas No.:122111-03-9

別名:鹽酸吉西他濱; LY 188011 hydrochloride

化學(xué)名: 4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride

Canonical SMILES:C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F

分子式:C9H11F2N3O4.HCI

分子量:299.66

溶解度:≥ 7.49mg/mL in Water; 25 mg/mL in DMSO (ultrasonic and warming and heat to 60°C)

儲存條件:4°C, protect from light

注意事項：

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References:

[1].Lansakara, P.D., B.L. Rodriguez, and Z. Cui, Synthesis and in vitro evaluation of novel lipophilic monophosphorylated gemcitabine derivatives and their nanoparticles. Int J Pharm, 2012. 429(1-2): p. 123-34.

[2].Kostyrev, O.A. and T.A. Leont'eva, [Autoradiographic study of DNA systhesis in muscle and connective tissue cells of the heart during exposure to isopropylnorepinephrine]. Biull Eksp Biol Med, 1973. 76(7): p. 108-11.

[3].Mathews, L.A., et al., Increased expression of DNA repair genes in invasive human pancreatic cancer cells. Pancreas, 2011. 40(5): p. 730-9.

[4].Banerjee, S., et al., Molecular evidence for increased antitumor activity of gemcitabine by genistein in vitro and in vivo using an orthotopic model of pancreatic cancer. Cancer Res, 2005. 65(19): p. 9064-72.