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Ixabepilone/伊沙匹隆 {[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/伊沙匹隆 化学结构 CAS号:219989-84-1
Ixabepilone/伊沙匹隆 化学结构
CAS号:219989-84-1
Ixabepilone/伊沙匹隆 3D分子结构
CAS号:219989-84-1
Ixabepilone/伊沙匹隆 化学结构 CAS号:219989-84-1
Ixabepilone/伊沙匹隆 3D分子结构 CAS号:219989-84-1
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Ixabepilone/伊沙匹隆 纯度/质量文件 产品仅供科研

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Ixabepilone/伊沙匹隆 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/伊沙匹隆 细胞实验

Cell Line
Concentration Treated Time Description References
Docetaxel-resistant MDA-MB-231 cells (TXT) 290 nM 48 hours Evaluate the effect of Ixabepilone on resistant cell viability, results showed Ixabepilone reduced cell viability to 34.2 ± 3.5% of control. Pharmacol Rep. 2022 Oct;74(5):998-1010.
MDA-MB-231 parental cells (231C) 22 nM 48 hours Evaluate the effect of Ixabepilone on cell viability, results showed Ixabepilone significantly reduced cell viability to 29.2 ± 2.0% of control. Pharmacol Rep. 2022 Oct;74(5):998-1010.
SUM159 5 nM 72 hours To evaluate the effect of Ixabepilone on cell viability. Results showed that Ixabepilone significantly reduced cell viability in a dose-dependent manner in SUM159 cells (IC50 = 8 ± 2 nM). Breast Cancer Res. 2016 Jan 12;18(1):6.
MDA-MB-231 5 nM 72 hours To evaluate the effect of Ixabepilone on cell viability. Results showed that Ixabepilone significantly reduced cell viability in a dose-dependent manner in MDA-MB-231 cells (IC50 = 10 ± 3 nM). Breast Cancer Res. 2016 Jan 12;18(1):6.
HOVTAX2 cells 10 nM 72 hours Evaluate the antitumor synergy of ixabepilone combined with sunitinib, results showed significant increase in apoptosis Gynecol Oncol. 2012 Mar;124(3):589-97.
Human lung cancer cell lines 2.3-19 nM (IC50) 72 hours Evaluate the cytotoxicity of Ixabepilone against various lung cancer cell lines, showing significant antitumor activity in most cell lines. Ther Adv Med Oncol. 2011 Jan;3(1):11-25.
Human colon cancer cell lines 4.7-42 nM (IC50) 72 hours Evaluate the cytotoxicity of Ixabepilone against various colon cancer cell lines, showing significant antitumor activity in most cell lines. Ther Adv Med Oncol. 2011 Jan;3(1):11-25.
Human breast cancer cell lines 1.4-45 nM (IC50) 72 hours Evaluate the cytotoxicity of Ixabepilone against various breast cancer cell lines, showing significant antitumor activity in most cell lines. Ther Adv Med Oncol. 2011 Jan;3(1):11-25.

Ixabepilone/伊沙匹隆 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
SCID/Beige mice MDA-MB-231 and SUM159 xenograft models Intraperitoneal injection 10 mg/kg Weekly To evaluate the effect of Ixabepilone on xenograft tumor growth. Results showed that Ixabepilone monotherapy significantly prolonged tumor doubling time (TDT = 25 ± 8 days) in SUM159 xenografts, but the effect was not significant in MDA-MB-231 xenografts. Breast Cancer Res. 2016 Jan 12;18(1):6.
Nu/nu mice or Beige SCID mice Human xenograft models (including NSCLC, breast cancer, and colon cancer) Intravenous 6-13 mg/kg (intravenous) Every 4 days for three doses Evaluate the antitumor activity of Ixabepilone alone or in combination with other anticancer agents, showing significant antitumor effects in various xenograft models, including tumor growth delay and partial or complete regression. Ther Adv Med Oncol. 2011 Jan;3(1):11-25.

Ixabepilone/伊沙匹隆 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/伊沙匹隆 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/伊沙匹隆 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/伊沙匹隆 技术信息

CAS号219989-84-1
分子式C27H42N2O5S
分子量 506.7
SMILES Code O=C(C[C@H](O)C1(C)C)N[C@H](/C(C)=C/C2=CSC(C)=N2)C[C@]3([H])O[C@]3(C)CCC[C@H](C)[C@H](O)[C@@H](C)C1=O
MDL No. MFCD04307791
别名 BMS-247550; Aza-epothilone B
运输蓝冰
InChI Key FABUFPQFXZVHFB-PVYNADRNSA-N
Pubchem ID 6445540
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place,Inert atmosphere,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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