Ixabepilone
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ixabepilone(BMS-247550)是一种埃博霉素B类似物,是一种口服生物可利用的微管抑制剂[1]。它与微管蛋白结合并促进微管蛋白聚合和微管稳定,从而使细胞停滞在细胞周期的G2-M期,并诱导肿瘤细胞凋亡[2]。
体外实验:在一系列肿瘤细胞系中,BMS-247550在诱导细胞毒性方面与埃博霉素B具有一样的活性。在测试的21个细胞系中,IC50值在1.4-34.5 nM之间。在浓度接近IC90(大约为7.5 nM,克隆形成细胞毒性实验)时,BMS-247550在药物处理开始后8小时几乎完全阻断有丝分裂中的细胞。
在体实验:BMS-247550在紫杉醇抗性和敏感性肿瘤中的抗肿瘤活性优于紫杉醇。在五个紫杉醇抗性肿瘤,如临床衍生的紫杉醇抗性Pat-7卵巢癌、由于微管蛋白突变对紫杉醇具有抗性的A2780Tax卵巢癌、HCT116/VM46MDR结肠癌、临床衍生的紫杉醇抗性Pat-21乳腺癌和鼠纤维肉瘤M5076中,BMS-247550比紫杉醇效果更好。在三种紫杉醇敏感性人肿瘤异种移植物,如A2780人卵巢癌、HCT116和LS174T人结肠癌中,BMS-247550具有与紫杉醇同等的抗肿瘤活性[2]。
临床试验:许多临床I期试验评估了与Ixabepilone相关的最佳剂量和毒性。基于早期试验中反应性和安全性的充分证据进行了二期临床研究,例如紫杉烷难治性乳腺癌患者、紫杉烷初始患者、紫杉烷初始和紫杉烷难治性的患者,和紫杉烷难治性患者[3]。
参考文献:
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
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.
Shannon Puhalla, Adam Brufsky. Ixabepilone: a new chemotherapeutic option for refractory metastatic breast cancer. Biologics. 2008 Sep; 2(3): 505–515.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 506.7 |
Cas No. | 219989-84-1 |
Formula | C27H42N2O5S |
Synonyms | Azaepothilone B; BMS 247550; BMS 247550-1; Ixempra |
Solubility | ≥22.25 mg/mL in DMSO; insoluble in H2O; ≥41.3 mg/mL in EtOH with gentle warming |
Chemical Name | (1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-((E)-1-(2-methylthiazol-4-yl)prop-1-en-2-yl)-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione |
SDF | Download SDF |
Canonical SMILES | C[C@H]([C@H](O)[C@@H](C)C(C(C)(C)[C@@H](O)C1)=O)CCC[C@]2(C)[C@@H](O2)C[C@@H](/C(C)=C/C3=CSC(C)=N3)NC1=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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