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伊沙匹隆 /Ixabepilone {[allProObj[0].p_purity_real_show]}

货号:A131078 同义名: BMS-247550;Aza-epothilone B

Ixabepilone是一种微管抑制剂,通过结合微管蛋白并促进其聚合和微管稳定化起作用。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Ixabepilone 化学结构 CAS号:219989-84-1
Ixabepilone 化学结构
CAS号:219989-84-1
Ixabepilone 3D分子结构
CAS号:219989-84-1
Ixabepilone 化学结构 CAS号:219989-84-1
Ixabepilone 3D分子结构 CAS号:219989-84-1
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Ixabepilone 纯度/质量文件 产品仅供科研

货号:A131078 标准纯度: {[allProObj[0].p_purity_real_show]}
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Ixabepilone 生物活性

描述 Ixabepilone is an epothilone analogue that shows cytotoxic potency against tumor cell lines with IC50 values ranging from 1.4 to 34.5 nM. The in vitro IC90 values of ixabepilone in HCT116, HCT/VM46, A2780S, and A2780Tax cells were 7.3, 16, 6.9 and 12 nM, respectively. Ixabepilone potently induced tubulin polymerization with an EC0.01 value of 3.5 μM. Eight-hour exposure of 7.5 nM ixabepilone almost completely blocked HCT116 cells in mitosis[1]. Ixabepilone inhibited cell viability in triple negative breast cancer cell lines with the IC50 values of 10 nM for MDA-MB-231 cells and 8 nM for SUM159 cells. After 72-hour incubation with 5 nM ixabepilone, the mammosphere formation in MDA-MB-231 and SUM159 cells were 0.21% and 0.30%, respectively. In immunocompromised nude rats implanted with Pat-7 tumor, i.v. administration of ixabepilone (3 mg/kg per injection) on a schedule of every 8 days × 2 elicited more than 5 log cell kill, and 4 of 6 cures. In A2780Tax human ovarian carcinoma xenograft, Iiabepilone (6.3 mg/kg per injection) on a schedule of every 2 days × 5 produced 2.5 log cell kill. In a paclitaxel-sensitive tumor model implanted with LS174T human colon carcinoma, ixabepilone (16 mg/kg per injection) administrated every 4 days × 3 yielded 2.3 log cell kill[2].
作用机制 The cellular cytotoxic activities of ixabepilone are linked to the induction of tubulin polymerization and the blockage of cell cycle progression in cancer cells[1].

Ixabepilone 动物研究

Dose Mice: 3.2 mg/kg - 10 mg/kg[3] (i.v.), 18.8 mg/kg - 150 mg/kg[4] (i.v.), 48 mg/kg (p.o.) Rat: 8 mg/kg[4] (p.o.)
Administration i.v., p.o.
Pharmacokinetics
Animal Mice[5]
Dose 10 mg/kg
Administration i.v.
MRT 3.62 h
AUCtot 5.77 μmol·h
T1/2α 0.204 h
T1/2β 9.23 h
CL 57.8 ml/min/kg
Cmax 14.7 μmol/L
Vss 46.2 L/kg

Ixabepilone 参考文献

[1]Lee FY, Borzilleri R, et al. BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy. Clin Cancer Res. 2001;7(5):1429-37.

[2]Tanei T, Choi DS, et al. Antitumor activity of Cetuximab in combination with Ixabepilone on triple negative breast cancer stem cells. Breast Cancer Res. 2016;18(1):6.

[3]Lee FY, Borzilleri R, et al. Preclinical discovery of ixabepilone, a highly active antineoplastic agent. Cancer Chemother Pharmacol. 2008 Dec;63(1):157-66.

[4]BMS2475501

[5]Peterson JK, Tucker C, et al. In vivo evaluation of ixabepilone (BMS247550), a novel epothilone B derivative, against pediatric cancer models. Clin Cancer Res. 2005 Oct 1;11(19 Pt 1):6950-8.

Ixabepilone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL

Ixabepilone 技术信息

CAS号219989-84-1
分子式C27H42N2O5S
分子量 506.698
别名 BMS-247550;Aza-epothilone B;Azaepothilone BBMS 2475501. Trade name: Ixempra.
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Room Temperature

溶解度

DMSO: 85 mg/mL(167.75 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

2% DMSO+30% PEG 300+2% Tween 80+water 7 mg/mL

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