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Ixabepilone

现货
Catalog No.
A3513
Epothilone B类似物,微管稳定剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 3,340.00
现货
5mg
¥ 3,150.00
现货

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Background

Ixabepilone(BMS-247550), an epothilone B analog, is an orally bioavailable microtubule inhibitor [1]. It could bind to tubulin and promote tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis[2].

In vitro: In a large panel of tumor cell lines, BMS-247550 was as active as epothilone B in inducing cytotoxicity. Of the 21 cells lines tested, the IC50 values were in the range of 1.4–34.5 nm. BMS-247550 almost completely blocked cells in mitosis as early as 8 h after the initiation of drug exposureat a concentration close to the IC90 (7.5 nm, clonogenic cytotoxicity assay) [2].

In vivo: BMS-247550 has clearly demonstrated antitumor activity that is superior to paclitaxel in both paclitaxel-sensitive and -resistant tumors. BMS-247550 was more efficacious than paclitaxel in all five paclitaxel-resistant tumors such as the clinically derived paclitaxel resistant Pat-7 ovarian carcinoma, the A2780Tax ovarian carcinoma that is resistant to paclitaxel because of tubulin mutations, the HCT116/VM46 MDR colon carcinoma, the clinically derived paclitaxel-resistant Pat-21 breast carcinoma, and the murine fibrosarcoma M5076. BMS-247550 produced antitumor activity equivalent to paclitaxel against three paclitaxel-sensitive human tumor xenografts such as A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma [2].

Clinical trials:Numerous phase I trials have evaluated the optimum dose and toxicity associated with ixabepilone. Various phase II studies were designed for patients with varying levels of previous therapies based on ample evidence of response and safety in early trials such as patients with taxane-refractory breast cancer, taxane-naive patients, both taxane-naive and taxane-refractory patients, taxane refractory patients[3].

References:
[1]. Lee FY1, Borzilleri R,Fairchild CR, Kim SH, Long BH, Reventos-Suarez C, Vite GD, Rose WC, Kramer RA.BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy. Clin Cancer Res.2001 May;7(5):1429-37
[2]. Denduluri N, Low J A, Lee J J, et al. Phase II trial of ixabepilone, an epothilone B analog, in patients with metastatic breast cancer previously untreated with taxanes[J]. Journal of clinical oncology, 2007, 25(23): 3421-3427.
[3]. Shannon Puhalla, Adam Brufsky. Ixabepilone: a new chemotherapeutic option for refractory metastatic breast cancer. Biologics. 2008 Sep; 2(3): 505–515.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt506.7
Cas No.219989-84-1
FormulaC27H42N2O5S
SynonymsAzaepothilone B; BMS 247550; BMS 247550-1; Ixempra
Solubility≥22.25 mg/mL in DMSO, ≥41.3 mg/mL in EtOH with gentle warming, <2.14 mg/mL in H2O
Chemical Name(1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione
SDFDownload SDF
Canonical SMILESCC1CCCC2(C(O2)CC(NC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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