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| 品牌 | absin | CAS | 75747-14-7 |
|---|---|---|---|
| 分子式 | C31H43N3O8 | 纯度 | >98 % |
| 分子量 | 585.7 | 货号 | abs810017 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | 是一种有效的HSP90抑制剂 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
17-AAG 75747-14-7
| 产品描述 | |
| 描述 | Tanespimycin (17-AAG)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。 |
| 纯度 | >98 % |
| 储存/保存方法 | Store at -20℃ for three years（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 坦螺旋mei素；替拉替尼；17-烯丙基胺格尔德霉素；Tanespimycin; NSC 330507; CP 127374; 17AAG; 17 AAG; KOS 953 |
| 外观 | Purple or dark red solid |
| 可溶性/溶解性 | DMSO : 58.6 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | HSP90 |
| In vitro(体外研究) | 17-AAG, an analog of geldanamycin, exhibits greater than 100 times higher binding affinity for Hsp90 derived from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells with IC50 values of 5-6 nM. 17-AAG causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells such as LNCaP, LAPC-4, DU-145, and PC-3 with IC50 values of 25-45 nM. In addition to inducing apoptosis of Ba/F3 cells transformed with wild-type BCR-ABL with an IC50 of 5.2 μM, 17-AAG has the ability to induce apoptosis of cells transformed with imatinib mesylate-resistant T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively, by inducing the degradation of both wild-type BCR-ABL protein and mutants. |
| In vivo(体内研究) | 17-AAG displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice with IC50 values of 8-35 nM as compared with that from the normal tissues with IC50 values of 200-600 nM. Administration of 17-AAG (~50 mg/kg) causes significant decline in AR, HER2, HER3, and Akt expression in a dose-dependent manner with >50% decline at dose of 50 mg/kg, resulting in the dose-dependent inhibition of androgen-dependent (CWR22) and -independent (CWR22R and CWRSA6) prostate cancer xenografts growth by 67%, 80% and 68% at dose of 50 mg/kg, respectively. |
| 研究领域 | |
| 研究领域 | CancerTumor biomarkersOther NeuroscienceProcesses Signal TransductionProtein TraffickingChaperonesHeat Shock Proteins Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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