生物活性
AUY922 (Luminespib,NVP-AUY922)是一种高效的HSP90抑制剂，在Hsp90 FP结合测定中的IC50 = 21 nM，并在体外抑制多种人类癌细胞系的增殖，GI50平均为9 nM。Luminespib (AUY-922, NVP-AUY922)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。
靶点信息
| HSP90α (Cell-free assay) | HSP90β (Cell-free assay) | | | |
| 13 nM | 21 nM | | | |
化学数据
| 目录号 | A10659 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 465.5 |
| Formula | C26H31N3O5 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 747412-49-3 |
| Synonyms | VER-52296, AUY-922 |
| SMILES | CCNC(=O)C1=C(/C(=C/2\C=C(C(=CC2=O)O)C(C)C)/ON1)C3=CC=C(C=C3)CN4CCOCC4 |
溶解度
| In vitro (25°C) | DMSO | Warmed: 86 mg/mL (184.72 mM) |
| Water | Insoluble |
| Ethanol | 29 mg/mL (62.28 mM) |
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 28 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 21.48 mL | 107.41 mL | 214.82 mL |
| 0.5 mM | 4.3 mL | 21.48 mL | 42.96 mL |
| 1 mM | 2.15 mL | 10.74 mL | 21.48 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
*The above data is based on the productmolecular weight 465.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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