IPI-504 (Retaspimycin hydrochloride)
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥2703.00 | 10-15工作日发货 | |
| 5mg | ￥1574.00 | 10-15工作日发货 | |
| 10mg | ￥2519.00 | 10-15工作日发货 | |
| 50mg | ￥6802.00 | 10-15工作日发货 | |
| 100mg | ￥9851.00 | 10-15工作日发货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
Retaspimycin hydrochloride（IPI-504），17-AAG的对苯二酚盐酸盐衍生物，是一种新型有效的和选择性的热休克蛋白90（Hsp90）抑制剂，与Hsp90氨基末端的ATP/ADP结合位点结合。作为17-AAG的高水溶性形式，IPI-504（溶解度>200 mg/mL）不需要提前溶于有机溶剂中，因此可高浓度运输。一旦进入体循环，IPI-504去质子化，转变为游离碱IPI-504，随后氧化为17-AAG。在几种肿瘤细胞系中，IPI-504有效抑制细胞增殖，IC50范围介于10-40 nmol/L之间。IPI-504还用于治疗胃肠道间质瘤、软组织肉瘤和非小细胞肺癌。
参考文献：
Britt Erika Hanson and David H Vesole. Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent. Expert Opin. Investi. Drugs (2009) 18(9): 1375-1383
David Siegel, Sundar Jagannath, David H. Vesole, Ivan Borello, Amitabha Mazumder, Constantine Mitsiades, Jill Goddard, Joi Dunbar, Emmanuel Normant, Julian Adams, David Grayzel, Kenneth C. Anderson and Paul Richardson. A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refractory multiple myeloma. Leukemia & Lymphoma, 2011; 52(12): 2308-2315
Ching Ching Leow, Jon Chesebrough, Karen T. Coffman, Christine A. Fazenbaker, John Gooya, David Weng, Steve Coats, Dowdy Jackson, Bahija Jallal and Yong Chang. Antitumor efficacy of IPI-504, a selective heat shock protein 90 inhibitor against human epidermal growth factor receptor 2-positive human xenograft models as a single agent and in combination with trastuzumab or lapatinib. Mol Cancer Ther 2009; 8: 2131-2141
产品性质
| 物理外观 | A solid |
| CAS号 | 857402-63-2 |
| 分子式 | C31H46ClN3O8 |
| 分子量 | 624.2 |
| 小分子别名 | Retaspimycin Hydrochloride |
| 化学名称 | [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6,20,22-trihydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16-oxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(22),8,12,14,18,20-hexaen-10-yl] carbamate;hydrochloride |
| 溶解度 | ≥26.1 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥100 mg/mL in EtOH with ultrasonic |
| SMILES | CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=C(C(=C2O)C1)NCC=C)O)C)OC)OC(=O)N)C)C)O)OC.Cl |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | Retaspimycin Hcl（IPI504 Hcl）是热休克蛋白90（HSP90）的小分子抑制剂，具有抗增殖和抗肿瘤活性。 |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 3 篇科研文献
- 1.Katayama K, Noguchi K, et al. "Heat shock protein 90 inhibitors overcome the resistance to Fms-like tyrosine kinase 3 inhibitors in acute myeloid leukemia." Oncotarget. 2018 Sep 28;9(76):34240-34258. PMID:30344940
- 2.Dhawan A, Nichol D, et al."Collateral sensitivity networks reveal evolutionary instability and novel treatment strategies in ALK mutated non-small cell lung cancer." Sci Rep. 2017 Apr 27;7(1):1232. PMID:28450729
- 3.Debruyne DN, Bhatnagar N, et al. "ALK inhibitor resistance in ALK(F1174L)-driven neuroblastoma is associated with AXL activation and induction of EMT." Oncogene. 2016 Jul 14;35(28):3681-91. PMID:26616860
沪公网安备 31011002003500