AR-42
产品说明书
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同义名 : | HDAC-42;OSU-HDAC42;OSU-42;NSC-736012;(S)-HDAC-42 |
| CAS号 : | 935881-37-1 | |
| 货号 : | A374120 | |
| 分子式 : | C18H20N2O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 312.363 | |
| MDL号 : | MFCD17676151 | |
| 存储条件： |
Pure form Inert atmosphere,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 9 mg/mL(28.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 45 mg/mL(144.06 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear PO 0.5% CMC-Na 28 mg/mL suspension |
| 生物活性 | |||
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| 靶点 |
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| 描述 | AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). It causes growth inhibition, cell-cycle arrest, apoptosis, and activates caspases-3/7. AR-42 also leads to hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. It exhibits cytotoxic effects against a variety of human cancer cell lines[1][2]. | ||
| 作用机制 | AR-42 is a phenylbutyrate-derived inhibitor which can chelate the Zn2+ ion.[1] | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01798901 | Adult Acute Myeloid Leukemia W... 展开 >>ith 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Del(5q) Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(15;17)(q22;q12) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Myeloid Leukemia Secondary Acute Myeloid Leukemia Untreated Adult Acute Myeloid Leukemia 收起 << | Phase 1 | Completed | - | United States, Ohio ... 展开 >> Cincinnati Children's Hospital Cincinnati, Ohio, United States, 45229 Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Arthur G. James Cancer Hospital and Solove Research Institute at Ohio State University Medical Center Columbus, Ohio, United States, 43210 收起 << |
| NCT01129193 | Adult Nasal Type Extranodal NK... 展开 >>/T-cell Lymphoma Anaplastic Large Cell Lymphoma Angioimmunoblastic T-cell Lymphoma Cutaneous B-cell Non-Hodgkin Lymphoma Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue Hepatosplenic T-cell Lymphoma Intraocular Lymphoma Nodal Marginal Zone B-cell Lymphoma Peripheral T-cell Lymphoma Post-transplant Lymphoproliferative Disorder Prolymphocytic Leukemia Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Mixed Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Adult Grade III Lymphomatoid Granulomatosis Recurrent Adult Hodgkin Lymphoma Recurrent Adult Immunoblastic Large Cell Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Adult T-cell Leukemia/Lymphoma Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Mycosis Fungoides/Sezary Syndrome Recurrent Small Lymphocytic Lymphoma Refractory Chronic Lymphocytic Leukemia Refractory Multiple Myeloma Stage III Adult Burkitt Lymphoma Stage III Adult Diffuse Large Cell Lymphoma Stage III Adult Diffuse Mixed Cell Lymphoma Stage III Adult Diffuse Small Cleaved Cell Lymphoma Stage III Adult Hodgkin Lymphoma Stage III Adult Immunoblastic Large Cell Lymphoma Stage III Adult Lymphoblastic Lymphoma Stage III Adult T-cell Leukemia/Lymphoma Stage III Chronic Lymphocytic Leukemia Stage III Cutaneous T-cell Non-Hodgkin Lymphoma Stage III Grade 1 Follicular Lymphoma Stage III Grade 2 Follicular Lymphoma Stage III Grade 3 Follicular Lymphoma Stage III Mantle Cell Lymphoma Stage III Marginal Zone Lymphoma Stage III Multiple Myeloma Stage III Mycosis Fungoides/Sezary Syndrome Stage III Small Lymphocytic Lymphoma Stage IV Adult Burkitt Lymphoma Stage IV Adult Diffuse Large Cell Lymphoma Stage IV Adult Diffuse Mixed Cell Lymphoma Stage IV Adult Diffuse Small Cleaved Cell Lymphoma Stage IV Adult Hodgkin Lymphoma Stage IV Adult Immunoblastic Large Cell Lymphoma Stage IV Adult Lymphoblastic Lymphoma Stage IV Adult T-cell Leukemia/Lymphoma Stage IV Chronic Lymphocytic Leukemia Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma Stage IV Grade 1 Follicular Lymphoma Stage IV Grade 2 Follicular Lymphoma Stage IV Grade 3 Follicular Lymphoma Stage IV Mantle Cell Lymphoma Stage IV Marginal Zone Lymphoma Stage IV Mycosis Fungoides/Sezary Syndrome Stage IV Small Lymphocytic Lymphoma Testicular Lymphoma Waldenstrom Macroglobulinemia 收起 << | Phase 1 | Completed | - | United States, Ohio ... 展开 >> The Ohio State University James Cancer Hospital Columbus, Ohio, United States, 43210 收起 << |
| NCT02569320 | Recurrent Plasma Cell Myeloma | Phase 1 | Suspended(Internal data analys... 展开 >>is) 收起 << | March 31, 2019 | United States, Ohio ... 展开 >> Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 收起 << |
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.20mL 0.64mL 0.32mL |
16.01mL 3.20mL 1.60mL |
32.01mL 6.40mL 3.20mL |
| 参考文献 |
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