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Onalespib

AT13387,AT 13387,AT-13387

AT13387是一种有效的，选择性Hsp90抑制剂，作用于A375细胞，IC50为18 nM，具有较长时间的抗肿瘤活性。

目录号
EY0339
EY0339
EY0339
EY0339
EY0339
纯度
99.25%
99.25%
99.25%
99.25%
99.25%
规格
1 mg
5 mg
10 mg
25 mg
50 mg
原价
460
960
1500
2100
3800
售价
460
960
1500
2100
3800
库存
现货
现货
现货
现货
现货
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  • 生物活性

    Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1 μM

  • 动物实验

    80 mg/kg 腹腔注射

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Lyons J, et al.Poser A217.
    [2] Courtin A,et al. Emergence of resistance to tyrosine kinase inhibitors in non-small-cell lung cancer can be delayed by an upfront combination with the HSP90 inhibitor onalespib. Br J Cancer. 2016 Oct 25;115(9):1069-1077. doi: 10.1038/bjc.2016.294.
    [3] Ferraldeschi R,et al. Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells. Cancer Res. 2016 May 1;76(9):2731-42. doi: 10.1158/0008-5472.CAN-15-2186.
    [4] Spiegelberg D,et al. Molecular imaging of EGFR and CD44v6 for prediction and response monitoring of HSP90 inhibition in an in vivo squamous cell carcinoma model. Eur J Nucl Med Mol Imaging. 2016 May;43(5):974-82. doi: 10.1007/s00259-015-3260-x.

    分子式
    C24H31N3O3    		 分子量
    409.52    		 CAS号
    912999-49-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    25 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT02474173 Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma Other: Laboratory Biomarker Analysis|Drug: Onalespib|Drug: Paclitaxel|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2016-01-01 2017-02-02
    NCT02572453 Anaplastic Large Cell Lymphoma, ALK-Positive|BCL6 Positive|Recurrent Anaplastic Large Cell Lymphoma|Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Mantle Cell Lymphoma|Refractory Anaplastic Large Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Mantle Cell Lymphoma Other: Laboratory Biomarker Analysis|Drug: Onalespib National Cancer Institute (NCI) Phase 2 2016-04-01 2017-02-17
    NCT02535338 Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer Drug: Erlotinib Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Onalespib|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1|Phase 2 2016-01-01 2017-01-31
    NCT02503709 Metastatic Malignant Solid Neoplasm|Unresectable Solid Neoplasm Drug: CDKI AT7519|Other: Laboratory Biomarker Analysis|Drug: Onalespib|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2016-04-01 2017-03-10
    NCT01685268 Prostate Cancer Drug: AT13387|Drug: abiraterone acetate|Drug: Prednisone Astex Pharmaceuticals Phase 1|Phase 2 2012-09-01 2016-09-06
    NCT02898207 Estrogen Receptor Negative|HER2/Neu Negative|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Metastatic Malignant Solid Neoplasm|Primary Peritoneal High Grade Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma|Unresectable Solid Neoplasm Other: Laboratory Biomarker Analysis|Drug: Olaparib|Drug: Onalespib|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2017-05-01 2017-03-10
    NCT02097225 BRAF V600E Mutation Present|BRAF V600K Mutation Present|Metastatic Malignant Solid Neoplasm|Recurrent Malignant Solid Neoplasm|Recurrent Melanoma|Stage III Skin Melanoma|Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma|Unresectable Solid Neoplasm Drug: Dabrafenib|Other: Laboratory Biomarker Analysis|Drug: Onalespib|Other: Pharmacological Study|Drug: Trametinib National Cancer Institute (NCI) Phase 1 2014-05-01 2017-03-13
    NCT02381535 Human Papillomavirus Infection|Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma|Stage III Oropharyngeal Squamous Cell Carcinoma|Stage IVA Hypopharyngeal Squamous Cell Carcinoma|Stage IVA Laryngeal Squamous Cell Carcinoma|Stage IVA Oral Cavity Squamous Cell Carcinoma|Stage IVA Oropharyngeal Squamous Cell Carcinoma|Stage IVB Hypopharyngeal Squamous Cell Carcinoma|Stage IVB Laryngeal Squamous Cell Carcinoma|Stage IVB Oral Cavity Squamous Cell Carcinoma|Stage IVB Oropharyngeal Squamous Cell Carcinoma Drug: Cisplatin|Radiation: Intensity-Modulated Radiation Therapy|Other: Laboratory Biomarker Analysis|Drug: Onalespib|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2015-09-01 2017-01-31

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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