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Irinotecan Sale

(Synonyms: 伊立替康; (+)-Irinotecan; CPT-11) 目录号 : GC11473

伊立替康 ((+)-Irinotecan) 是一种拓扑异构酶 I 抑制剂,通过与拓扑异构酶 I-DNA 复合物结合来阻止 DNA 链的重新连接。

Irinotecan Chemical Structure

Cas No.:97682-44-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥410.00
现货
100mg
¥357.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment [1]:

Cell lines

HT29, NMG64/84, COLO-357, MIA PaCa-2 and PANC-1 cells

Preparation method

The solubility of this compound in DMSO is >29.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1-1000 μg/ml, 30 min

Applications

Irinotecan displayed concentration- and time-dependent cytotoxic effects in all tested cell lines. In COLO-357, MIA PaCa-2 and PANC-1 cells, irinotecan increased cell number in G0/G1 and decreased cell number in S- and G2-phase. Low concentration of irinotecan increased cell number in G2-phase in HT29 and NMG 64/84.

Animal experiment [2]:

Animal models

ICR male mice

Dosage form

Intraperitoneal injection, 100 mg/kg

Application

The time course of body weight change after Irinotecan (100 mg/kg i.p.) injection showed a significant dosing time-dependent difference (P

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. HOFMANN C, BUTTENSCHOEN K, STRAETER J, et al. Pre-clinical evaluation of the activity of irinotecan as a basis for regional chemotherapy[J]. Anticancer research, 2005, 25(2A): 795-804.

[2]. Ohdo S, Makinosumi T, Ishizaki T, et al. Cell cycle-dependent chronotoxicity of irinotecan hydrochloride in mice[J]. Journal of Pharmacology and Experimental Therapeutics, 1997, 283(3): 1383-1388.

产品描述

Irinotecan (CPT-11), a prodrug for treating metastatic colorectal cancer, is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively [1].In vivo, Irinotecan is converted to SN-38, its most active metabolite, by carboxylesterase converting enzyme (CCE) [2].

In vitro: Irinotecan induced similar amounts of cleavable complexes in LoVocells and HT-29 cell lines with the IC50 of 15.8 μM and 5.17 μM, respectively [1].After addition of 157 mM irinotecan to plasma, SN-38 concentration showed linear increase during the first 60-min period, followed by a plateau.In the first 60 min, mean and standard deviation of the conversion rate were 515.9 ± 50.1 pmol/ml/h (n = 69), with a coefficient of variation of 0.097 [2]. Irinotecan (CPT-11) was significantly more active in SCLC than in NSCLCcelllines (P = 0.0036). CE activity appeared to be associated with higher sensitivity to CPT-11 in human lung cancercelllines and may partly explain the difference in the in vitro sensitivity to CPT-11 between SCLC and NSCLCcells [3].In vitro, the sensitivity to CPT-11 and SN-38 was highest in LS174T and COLO 320cells, intermediate in SW1398cellsand lowest in COLO 205 and WiDr cells. The activity of SN-38 was 130 to 570 times than CPT-11[4].

In vivo: In COLO 320 xenografts, Irinotecan induced a maximum growth inhibition of 92% [4].A single dose of Irinotecan significantly increased amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver. Concomitantly, the Irinotecan-treated group exihibited significantly higher amounts of DNA strand breaks in colon mucosa cells compared to the control group [5].

伊立替康(CPT-11)是治疗转移性结直肠癌的一种前药,是拓扑异构酶I的抑制剂,在LoVo细胞和HT-29细胞中的IC50分别为15.8μM和5.17μM[1]。在体内,伊立替康通过羧酯酶转换酶(CCE)转化为其最活跃的代谢物SN-38[2]。

在体外,伊立替康在LoVo和HT-29细胞系中诱导相似量的可断链复合物,IC50分别为15.8μM和5.17μM[1]。157 mM伊立替康加入血浆后,SN-38浓度在前60分钟内呈线性增加,之后进入稳定期。前60分钟内,平均转化速率为515.9±50.1 pmol/ml/h(n=69),变异系数为0.097 [2]。伊立替康(CPT-11)在小细胞肺癌(SCLC)细胞系中比非小细胞肺癌(NSCLC)细胞系更为活跃(P = 0.0036)。羧酯酶活性似乎与人类肺癌细胞系对CPT-11的敏感性更高有关,这可能部分解释了SCLC和NSCLC细胞系之间在体外敏感性差异[3]。在体外,LS174T和COLO 320细胞的对CPT-11和SN-38的敏感性最高,SW1398细胞的敏感性居中,COLO 205和WiDr细胞的敏感性最低。SN-38的活性是CPT-11的130到570倍[4]。

在体内,伊立替康在COLO 320移植瘤中诱导最大92%的生长抑制[4]。单次伊立替康剂量显著增加胃、十二指肠、结肠和肝脏中与DNA共价结合的拓扑异构酶I量。同时,与对照组相比,伊立替康治疗组结肠粘膜细胞中的DNA链断裂量显著增加[5]。

References:
[1].  Tobin P, Clarke S, Seale J P, et al. The in vitro metabolism of irinotecan (CPT‐11) by carboxylesterase and β‐glucuronidase in human colorectal tumours[J]. British journal of clinical pharmacology, 2006, 62(1): 122-129.
[2]. Shingyoji M, Takiguchi Y, Watanabe‐Uruma R, et al. In vitro conversion of irinotecan to SN‐38 in human plasma[J]. Cancer science, 2004, 95(6): 537-540.
[3]. van Ark-Otte J, Kedde M A, Van Der Vijgh W J, et al. Determinants of CPT-11 and SN-38 activities in human lung cancer cells[J]. British journal of cancer, 1998, 77(12): 2171.
[4]. Jansen W J M, Zwart B, Hulscher S T M, et al. CPT-11 in human colon-cancer cell lines and xenografts: characterization of cellular sensitivity determinants[J]. International journal of cancer, 1997, 70(3): 335-340.
[5]. Na Y S, Jung K A, Kim S M, et al. The histone deacetylase inhibitor PXD101 increases the efficacy of irinotecan in in vitro and in vivo colon cancer models[J]. Cancer chemotherapy and pharmacology, 2011, 68(2): 389-398.

Chemical Properties

Cas No. 97682-44-5 SDF
别名 伊立替康; (+)-Irinotecan; CPT-11
化学名 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
Canonical SMILES O=C(OC1)C(O)(CC)C2=C1C(N(CC3=C4N=C5C(C=C(OC(N6CCC(N7CCCCC7)CC6)=O)C=C5)=C3CC)C4=C2)=O
分子式 C33H38N4O6 分子量 586.68
溶解度 >29.4mg/mL in DMSO 储存条件 4°C, protect from light
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 1.7045 mL 8.5225 mL 17.0451 mL
5 mM 0.3409 mL 1.7045 mL 3.409 mL
10 mM 0.1705 mL 0.8523 mL 1.7045 mL
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