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外観
白色～わずかにうすい褐色, 結晶～粉末
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溶解性
アセトンに溶けやすく、エタノールにやや溶けやすく、水にほとんど溶けない。
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用途
タキソイド系化合物です。細
胞内でチューブリンの重合を促進し、脱重合
を阻害することにより、細胞の有糸分裂停止
作用を示します。
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用途
タキソイド系化合物です。細
胞内でチューブリンの重合を促進し、脱重合
を阻害することにより、細胞の有糸分裂停止
作用を示します。
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効能
抗悪性腫瘍薬, 微小管脱重合阻害薬
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説明
Docetaxel, a semi-synthetic product from the taxoid family, was launched in
1995 first in South Africa and subsequently in several other markets for the treatment of
ovarian, breast and non-small cell lung cancers. Like the naturally occurring antitumor
agent paclitaxel, the first marketed taxoid, docetaxel promotes both the rate and extent
of tubulin assembly into stable microtubules and inhibits their depolymerization. It acts
as a mitotic spindle poison and induces a mitotic block in proliferating cells. This
mechanism of action for taxoids is unique from other classes of anticancer agents.
Docetaxel was reported to be twice as potent as paclitaxel in several in vitro protocols
and also exhibit higher cytotoxicity. Clinical trials are on going for docetaxel for other
types of tumors including pancreatic, gastric, head and neck cancers and soft tissue
sarcomas.
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化学的特性
Off-white Cryst
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使用
Docetaxel is a semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM). It has proven more effective than taxol in preventing the proliferation of cancer cells. Docetaxel has applications in breast cancer and hormone-refractory prostate cancer. This product is intended for research applications.
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定義
ChEBI: A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.
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危険性
A poison. Human systemic effects.
