セリチニブ

化学名:セリチニブ

英語名:Ceritinib (LDK378)

CBNumberCB82652832

MFC28H36ClN5O3S

MW558.14

别名

セリチニブ

セリチニブ (JAN)

5-クロロ-N′-[2-[(1-メチルエチル)スルホニル]フェニル]-N-[5-メチル-2-(1-メチルエトキシ)-4-(4-ピペリジニル)フェニル]-2,4-ピリミジンジアミン

セリチニブ物理性質

融点	173-175°C
沸点	720.7±70.0 °C(Predicted)
比重(密度)	1.251±0.06 g/cm3(Predicted)
貯蔵温度	-20°C Freezer
溶解性	クロロホルム（微量）、メタノール（微量）
酸解離定数(Pka)	10.16±0.10(Predicted)
外見	オフホワイトの固体。
色	ホワイトからオフホワイト
InChIKey	VERWOWGGCGHDQE-UHFFFAOYSA-N
SMILES	C1(NC2=CC(C)=C(C3CCNCC3)C=C2OC(C)C)=NC=C(Cl)C(NC2=CC=CC=C2S(C(C)C)(=O)=O)=N1

危険有害性情報のコード(GHS)

製品番号	包装	価格	製品説明	購入
富士フイルム和光純薬株式会社(wako) W01COBQJ-9413	100mg	￥644400		購入

効能
抗悪性腫瘍薬, 未分化リンパ腫キナーゼ(ALK)阻害薬
商品名
ジカディア (ノバルティスファーマ)
説明
Ceritinib (previously LDK378l, brand name Zykadia; Novartis Pharmaceuticals) is an oral small molecule tyrosine kinase inhibitor of ALK [87]. Preclinical studies suggested that it would inhibit ROS1 as well [88, 89].
使用
5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine, is a Anaplastic lymphoma kinase (ALK) inhibitor.
適応症
Ceritinib (Zykadia(R), Novartis), approved in 2014, was developed as a second-generation ALK inhibitor for patients with NSCLC who have developed crizotinib resistance. Ceritinib addresses two of the most common ALK mutants that lead to crizotinib resistance, L1196M andG1269A, but is ineffective for G1202R and F1174C variants of ALK.
定義
ChEBI: A member of the class of aminopyrimidines that is 2,6-diamino-5-chloropyrimidine in which the amino groups at positions 2 and 6 are respectively carrying 2-methoxy-4-(piperidin-4-yl)-5-methylphenyl and 2-(isopropylsulfonyl)phenyl substituents. Used for the treatment of ALK-positive metastatic non-small cell lung cancer.
一般的な説明
Class: receptor tyrosine kinase; Treatment: NSCLC; Elimination half-life = 41 h; Protein binding = 97%
製品名
Zykadia

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