酸伊立替康三水合物(CPT-11)是喜樹堿的半合成衍生物，對(duì)P388白血病的IC50值為3.4 μm[1]。 合成CPT-11以避免毒性并提高喜樹堿的治療效果。FDA已批準(zhǔn)其用于治療結(jié)腸或直腸轉(zhuǎn)移性癌患者，其疾病在基于5-氟尿嘧啶的治療后復(fù)發(fā)或進(jìn)展。CPT-11是SN-38的可溶性前藥，它在體內(nèi)被羧酸酯酶轉(zhuǎn)化為SN-38。SN-38是拓?fù)洚悩?gòu)酶I的有效抑制劑[2]。 發(fā)現(xiàn)CPT-11對(duì)耐藥性和藥物敏感性腫瘤細(xì)胞具有療效。它抑制對(duì)VCR或ADM耐藥的腫瘤的生長(zhǎng)。這種抑制也可能發(fā)生在對(duì)VCR和ADM耐藥的荷瘤小鼠中[1]。

產(chǎn)品性質(zhì)：

Cas No.:136572-09-3

別名:鹽酸伊立替康三水合物; (+)-Irinotecan hydrochloride trihydrate; CPT-11 hydrochloride trihydrate

化學(xué)名: (S)-4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl [1,4'-bipiperidine]-1'-carboxylate hydrochloride trihydrate

Canonical SMILES O=C(N1CCC(CC1)N2CCCCC2)OC3=CC4=C(CC)C5=C(C(N6C5)=CC(C7(CC)O)=C(COC7=O)C6=O)N=C4C=C3.Cl.O.O.O

分子式:C33H45ClN4O9

分子量:677.18

溶解度:≥ 23.1mg/mL in DMSO, ≥ 2.5mg/mL in Water

儲(chǔ)存條件:Store at -20°C

注意事項(xiàng)：

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References:

[1] Tsuruo T, Matsuzaki T, Matsushita M, Saito H, Yokokura T. Antitumor effect of CPT-11, a new derivative of camptothecin, against pleiotropic drug-resistant tumors in vitro and in vivo. Cancer Chemother Pharmacol. 1988;21(1):71-4.

[2] Slatter JG, Schaaf LJ, Sams JP, Feenstra KL, Johnson MG, Bombardt PA, Cathcart KS, Verburg MT, Pearson LK, Compton LD, Miller LL, Baker DS, Pesheck CV, Lord RS 3rd. Pharmacokinetics, metabolism, and excretion of irinotecan (CPT-11) following I.V. infusion of [(14)C]CPT-11 in cancer patients. Drug Metab Dispos. 2000 Apr;28(4):423-33.