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| | 1-シクロプロピル-3-[3-[5-(モルホリノメチル)-1H-ベンゾイミダゾール-2-イル]-1H-ピラゾール-4-イル]尿素 製品概要 |
| 化学名: | 1-シクロプロピル-3-[3-[5-(モルホリノメチル)-1H-ベンゾイミダゾール-2-イル]-1H-ピラゾール-4-イル]尿素 | | 英語化学名: | AT9283 | | 别名: | 1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea AT9283;AT9283, >=98%;N-cyclopropyl-N'-[3-[5-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]Urea;Urea, N-cyclopropyl-N'-[3-[6-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]-;1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea;CS-48;AT-9283; AT 9283;J-504568 | | CAS番号: | 896466-04-9 | | 分子式: | C19H23N7O2 | | 分子量: | 381.43 | | EINECS: | | | カテゴリ情報: | Inhibitor;Inhibitors | | Mol File: | 896466-04-9.mol | ![1-シクロプロピル-3-[3-[5-(モルホリノメチル)-1H-ベンゾイミダゾール-2-イル]-1H-ピラゾール-4-イル]尿素](CAS/GIF/896466-04-9.gif) |
| | 1-シクロプロピル-3-[3-[5-(モルホリノメチル)-1H-ベンゾイミダゾール-2-イル]-1H-ピラゾール-4-イル]尿素 物理性質 |
| 比重(密度) | 1.45 | | 貯蔵温度 | under inert gas (nitrogen or Argon) at 2–8 °C | | 溶解性 | insoluble in H2O; ≥19.05 mg/mL in DMSO; ≥47.6 mg/mL in EtOH with ultrasonic | | 外見 | solid | | 酸解離定数(Pka) | 10.58±0.10(Predicted) |
| | 1-シクロプロピル-3-[3-[5-(モルホリノメチル)-1H-ベンゾイミダゾール-2-イル]-1H-ピラゾール-4-イル]尿素 Usage And Synthesis |
| 使用 | AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC50s = 3, 3, 1.2, 1.1, and 4 nM, respectively). It also potently (IC50 = <1 μM) inhibits many other kinases, including serine/threonine kinases as well as receptor and non-receptor tyrosine kinases. As Aurora kinases have roles in mitosis, inhibitors of these kinases, including AT-9283, have potential in cancer therapy. Consistent with this, AT-9283 is effective in preventing proliferation of cancer cells both in vitro and in vivo and this effect may be enhanced by combination therapy with other chemotherapeutics.[Cayman Chemical] | | 定義 | ChEBI: 1-cyclopropyl-3-[3-[5-(4-morpholinylmethyl)-2-benzimidazolylidene]-1,2-dihydropyrazol-4-yl]urea is a member of benzimidazoles. | | 生物活性 | at9283, a synthetic small heterocyclic molecule discovered using a fragment-based approach, is a novel inhibitor of aurora kinase, a family of serine/threonine kinases regulating both mitosis and meiosis, that potently inhibits aurora kinases a and b, with 50% inhibition concentration ic50 value of 3 nm, as well as janus kinases (jaks), abelson kinase (bcrabl t315i) and flt-3. at9283 has been found to be therapeutic in leukemic cells, myeloproliferative disorders and multiple solid tumor cell lines. study results have shown that at9283 exhibits anti-proliferative activity and induces polyploidy and apoptosis in aggressive b-cell nhl cell lines associated with inhibition of aurora kinase b.qi w, liu x, cooke ls, persky do, miller tp, squires m, mahadevan d. at9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive b-cell lymphomas. int j cancer. 2012 jun 15;130(12):2997-3005. doi: 10.1002/ijc.26324. epub 2011 nov 19.arkenau ht, plummer r, molife lr, olmos d, yap ta, squires m, lewis s, lock v, yule m, lyons j, calvert h, judson i. a phase i dose escalation study of at9283, a small molecule inhibitor of aurora kinases, in patients with advanced solid malignancies. ann oncol. 2012 may;23(5):1307-13. doi: 10.1093/annonc/mdr451. epub 2011 oct 19. | | target | Aurora A |
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