Ganetespib (STA-9090)
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.
Ganetespib（STA-9090，5-[2,4-dihydroxy-5-(1 methylethyl)phenyl]-2,4 dihydro-4-(1-methyl-
1H indol-5 yl)-3H-1,2,4 triazole-3-one）是一种有效的热休克蛋白90（Hsp90）小分子抑制剂，与Hsp90 N端的ATP口袋结合，导致Hsp90客户蛋白水平的下调。与geldanamycin衍生的Hsp90抑制剂（17-AAG、17-DMAG和IPI-504）结构上不相关，ganetespib具有独特的含三唑酮的化学结构，在效力、抗肿瘤活性和安全性方面比其它Hsp90抑制剂更突出。据报道，ganetespib对广泛的人类癌症均具有抗肿瘤活性，包括肺癌、前列腺癌、结肠癌、乳腺癌、黑色素瘤和白血病。
参考文献：
Weiwen Ying, Zhenjian Du, Lijun Sun, Kevin P. Foley, David A. Proia, Ronald K. Blackman, Dan Zhou, Takayo Inoue, Noriaki Tatsuta, Jim Sang, Shuxia Ye, Jamie Acquaviva, Luisa Shin Ogawa, Yumiko Wada, James Barsoum, and Keizo Koya. Ganetespib, a unqiue triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther 2012; 11: 475-484
Jonathan W Goldman, Robert N Raju, Gregory A Gordon, Iman El-Hariry, Florentina Teofilivivi, Vojo M Vukovic, Robert Bradley, Michael D Karol, Yu Chen, Wei Guo, Takayo Inoue and Lee Rosen. A first in human, safety, pharmacokinetics, and clinical activity phase I study of once weekly administration of the Hsp90 inhibitor ganetespib (STA-9090) in patients with solid malignancies. BMC Cancer 2013; 13:152
- 1. Shuai Zhao, Lanlan Zhou, et al. "Anti-cancer efficacy including Rb-deficient tumors and VHL-independent HIF1α proteasomal destabilization by dual targeting of CDK1 or CDK4/6 and HSP90." Sci Rep. 2021 Oct 22;11(1):20871. PMID:34686682
- 2. Diwei Zheng, Weihai Liu, et al. "AHA1 upregulates IDH1 and metabolic activity to promote growth and metastasis and predicts prognosis in osteosarcoma." Signal Transduct Target Ther. 2021 Jan 20;6(1):25. PMID:33468990
- 3. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758
- 4. Karney-Grobe S, Russo A, et al. "HSP90 is a chaperone for DLK and is required for axon injury signaling." Proc Natl Acad Sci U S A. 2018 Oct 16;115(42):E9899-E9908. PMID:30275300
- 5. Khurana N, Kim H, et al. "Multimodal actions of the phytochemical sulforaphane suppress both AR and AR-V7 in 22Rv1 cells: Advocating a potent pharmaceutical combination against castration-resistant prostate cancer." Oncol Rep. 2017 Aug 30. PMID:28901514
- 6. Li QQ, Hao JJ,et al. "Proteomic analysis of proteome and histone post-translational modifications in heat shock protein 90 inhibition-mediated bladder cancer therapeutics." Sci Rep. 2017 Mar 15;7(1):201. PMID:28298630
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 364.4 |
| Cas No. | 888216-25-9 |
| Formula | C20H20N4O3 |
| Synonyms | STA9090, STA 9090 |
| Solubility | insoluble in H2O; ≥18.22 mg/mL in DMSO; ≥6.4 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | (5Z)-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-(1-methylindol-5-yl)-1,2,4-triazolidin-3-one |
| SDF | Download SDF |
| Canonical SMILES | CC(C)C1=CC(=C2NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)C(=O)C=C1O |
| 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。 |
| 细胞实验 [1]: | |
|
细胞系 |
NCI-H1975和HCC827细胞 |
|
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
0.001 ~ 1 μM；5、15或60分钟或24小时 |
|
实验结果 |
在NCI-H1975和HCC827细胞中，使用Ganetespib处理细胞，只需60分钟即可以产生细胞毒性，其IC50值分别为510 nM和800 nM。在NCI-H1975细胞中，使用Ganetespib处理细胞，5分钟足以产生少于1 μM的IC50值。 |
| 动物实验 [1]: | |
|
动物模型 |
NCI-H1395非小细胞肺癌异种移植小鼠模型 |
|
给药剂量 |
150 mg/kg；静脉注射；每周1次 |
|
实验结果 |
Ganetespib诱导NCI-H1395肿瘤消退，其T/C值为-49%。 |
|
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Weiwen Ying, Zhenjian Du, Lijun Sun, Kevin P. Foley, David A. Proia, Ronald K. Blackman, Dan Zhou, Takayo Inoue, Noriaki Tatsuta, Jim Sang, Shuxia Ye, Jamie Acquaviva, Luisa Shin Ogawa, Yumiko Wada, James Barsoum, and Keizo Koya. Ganetespib, a unqiue triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther 2012; 11: 475-484. |
|
| 描述 | Ganetespib (STA-9090)是HSP90的抑制剂，在OSA 8细胞中的IC50值为4 nM。 | |||||
| 靶点 | HSP90 | |||||
| IC50 | 4 nM | |||||
质量控制和MSDS
- 批次:
化学结构
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