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| 化学名: | BIIB 021 | | 英語化学名: | BIIB-021 | | 别名: | CNF2024;9-[2-(2,2-diMethyl-propylaMino)ethyl]-8-(2-iodo-5-Methoxy-phenylsulfanyl)-9H-purin-6-ylaMine;CNF-2024EC102;9H-Purin-2-aMine, 6-chloro-9-[(4-Methoxy-3,5-diMethyl-2-pyridinyl)Methyl]-;6-chloro-9-((4-Methoxy-3,5-diMethylpyridin-2-yl)Methyl)-9H-purin-2-aMine;BIIB-021;BIIB021/CNF2024;6-Chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine | | CAS番号: | 848695-25-0 | | 分子式: | C14H15ClN6O | | 分子量: | 318.76 | | EINECS: | 812-781-2 | | カテゴリ情報: | Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Antineoplastic;Inhibitor | | Mol File: | 848695-25-0.mol |  |
| 融点 | 192-193℃ | | 沸点 | 588.5±60.0 °C(Predicted) | | 比重(密度) | 1.50 | | 貯蔵温度 | -20°C | | 溶解性 | Soluble in DMSO (>25 mg/ml) | | 外見 | solid | | 酸解離定数(Pka) | 6.07±0.40(Predicted) | | 色 | White | | 安定性： | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 montha. |
| | BIIB 021 Usage And Synthesis |
| 溶解性 | In vitro (25℃) DMSO 64 mg/mL (200.77 mM) | | 説明 | BIIB021 is a potent HSP90 inhibitor (IC50 = 30 nM HER-2 degradation).1 It inhibited the proliferation of MCF7 and BT474 breast cancer cell lines (IC50 = 100 nM for each).? BIIB021 has shown efficacy as a therapeutic in multiple cancer models.2-5 | | 使用 | BIIB 021 an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Studies show that BIIB 021 adminisitration led to degradation of Hsp90 client proteins measured in tumor tissue and resulted in the inhibition of tumor growth in several human tumor xenograft models. | | 定義 | ChEBI: A member of the class of 2-aminopurines that is 2-aminopurine which is substituted by a chlorine at position 6 and by a (4-methoxy-3,5-dimethylpyridin-2-yl)methyl group at position 9. | | 参考文献 | Kasibhatla et al. (2007), Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity; J. Med. Chem. 50 2767
Lundgren et al. (2009), BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90; Mol. Cancer Ther. 8 921
Boll et al. (2009), Heat shock protein 90 inhibitor BIIB021 (CNF2024) depletes NF-kappaB and sensitizes Hodgkin’s lymphoma cells for natural killer cell-mediated cytotoxicity; Clin. Cancer Res. 15 5108
Zhang et al. (2010), BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance; Int. J. Cancer 126 1226
Wang et al. (2014), BIIB021, a novel Hsp90 inhibitor, sensitizes esophageal squamous cell carcinoma to radiation; Biochem. Biophys. Res. Commun. 452 945 |
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