ピクサントロン
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- CAS番号.
- 144510-96-3
- 化学名:
- ピクサントロン
- 别名:
- ピクサントロン;6,9-ビス[(2-アミノエチル)アミノ]-5H,10H-ベンゾ[g]イソキノリン-5,10-ジオン;6,9-ビス(2-アミノエチルアミノ)-5,10-ジヒドロベンゾ[g]イソキノリン-5,10-ジオン;ピキサントロン;6,9-ビス[(2-アミノエチル)アミノ]ベンゾ[g]イソキノリン-5,10-ジオン
- 英語名:
- Pixantrone
- 英語别名:
- CS-1359;pixantrone;Pixantrone, BBR 2778;BBR-2778;BBR2778;BBR 2778;Pixantrone diformate salt;6,9-Bis[(2-aminoethyl)amino]benz[g]isoquinoline-5,10-dione;6,9-bis((2-aminoethyl)amino)benzo(g)isoquinoline-5,10-dione;Benz[g]isoquinoline-5,10-dione, 6,9-bis[(2-aminoethyl)amino]-
- CBNumber:
- CB71321822
- 化学式:
- C17H19N5O2
- 分子量:
- 325.37
- MOL File:
- 144510-96-3.mol
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ピクサントロン 物理性質
- 融点 :
- >173°C (dec.)
- 沸点 :
- 650.0±55.0 °C(Predicted)
- 比重(密度) :
- 1.405
- 貯蔵温度 :
- Refrigerator
- 溶解性:
- DMSO（微量）、メタノール（微量）
- 酸解離定数(Pka):
- 9.34±0.10(Predicted)
- 外見 :
- 個体
- 色:
- ダークブルーからベリーダークブルー
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
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| 注意喚起語 |
警告 |
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
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P264, P270, P301+P312, P330, P501 |
| H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
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P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
強い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
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P264, P280, P305+P351+P338,P337+P313P |
| H335 |
呼吸器への刺激のおそれ |
特定標的臓器毒性、単回暴露； 気道刺激性 |
3 |
警告 |
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| 注意書き |
| P261 |
粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。 |
| P305+P351+P338 |
眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
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ピクサントロン 価格
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
ピクサントロン 化学特性,用途語,生産方法
効能
抗悪性腫瘍薬, トポイソメラーゼII阻害薬
説明
In May 2012, pixantrone was approved by the European Commission as a single agent for the treatment of relapsed or refractory aggressive B-cell non-Hodgkin lymphoma (NHL) in adult patients who have failed on at least two previous therapies. Pixantrone (also known as BBR- 2778) is an anthracycline analogue that was specifically designed to address the cardiotoxicity seen in earlier agents by replacement of a 1,4- dihydroxyanthracene-9,10-dione core with a benzoisoquinoline-5,10-dione ring system. Pixantrone inhibits topoisomerase II by intercalation with DNA and is also believed to form covalent adducts with the N-2 amino group of guanine via a formaldehyde aminal formed with the primary amino groups. Pixantrone is less cytotoxic than other anthracycline derivatives, but shows good antitumor activity in vivo in a variety of preclinical tumor models, including leukemia and lymphoma models. Pixantrone also demonstrated significantly reduced cardiotoxicity in preclinical models compared with the anthracyclines doxorubicin and mitroxantrone. Pixantrone was synthesized by Friedel–Crafts reaction of pyridine-3,4-dicarboxylic acid anhydride with 1,4-difluorobenzene to give a ketoacid that was cyclized to the tricyclic core by treatment with fuming sulfuric acid at 140℃. Reaction of the resulting 6,9-difluorobenzoisoquinoline-5-10-dione with ethylenediamine followed by careful pH adjustment and treatment with maleic acid gave pixantrone in good overall yield and purity.
使用
Pixantrone is an antineoplastic drug belonging to group of antitumor antibiotics. Pixantrone is an anlogue of Mitoxantrone (M373425) and is just as potent in the treatment of multiple sclerosis with fewer toxic effects on cardiac tissue. Studies suggest that Pixantrone significantly reduces amyloid beta (A beta(1-42)) neurotoxicity, a mechanism implicated in Alzheimer's disease.
臨床応用
Pixuvri (Pixantrone dimaleate) is a novel aza-anthracenedione derivative approved in Europe for the
treatment of adult patients with non-Hodgkin B-cell lymphoma. It is also being pursued as a
treatment for various cancers, and specifically as an alternative to other structurally-related drugs like
mitoxantrone, employed for treatment of breast cancer, acute myeloid leukemia (AML), and non-
Hodgkins lymphoma.Pixantrone dimaleate has been designed to maintain antitumor efficacy while
decreasing highly cardiotoxic side effects observed during treatment with other related anti-tumor
anthracenedione derivatives. Like many anthracenedione drugs, the mechanism of action for pixantrone dimaleate likely includes a number of pathways and processes, with studies suggesting
intercalation into DNA and/or interference with DNA –Topoisomerase II activity, leading to subsequent
protein associated-DNA strand breaks and eventually to cell death.
ピクサントロン 上流と下流の製品情報
原材料
準備製品
ピクサントロン 生産企業
Global( 99)Suppliers
144510-96-3(ピクサントロン)キーワード:
- 144510-96-3
- 6,9-bis((2-aminoethyl)amino)benzo(g)isoquinoline-5,10-dione
- pixantrone
- 6,9-Bis[(2-aminoethyl)amino]benz[g]isoquinoline-5,10-dione
- CS-1359
- Pixantrone, BBR 2778
- BBR-2778;BBR2778;BBR 2778
- Benz[g]isoquinoline-5,10-dione, 6,9-bis[(2-aminoethyl)amino]-
- Pixantrone diformate salt
- ピクサントロン
- 6,9-ビス[(2-アミノエチル)アミノ]-5H,10H-ベンゾ[g]イソキノリン-5,10-ジオン
- 6,9-ビス(2-アミノエチルアミノ)-5,10-ジヒドロベンゾ[g]イソキノリン-5,10-ジオン
- ピキサントロン
- 6,9-ビス[(2-アミノエチル)アミノ]ベンゾ[g]イソキノリン-5,10-ジオン