ラパチニブ

化学名:ラパチニブ

CAS番号.231277-92-2

英語名:Lapatinib

CBNumberCB8855402

MFC29H26ClFN4O4S

MW581.06

MOL File231277-92-2.mol

别名

ラパチニブ

4-[[4-(3-フルオロベンジルオキシ)-3-クロロフェニル]アミノ]-6-[5-[[[2-(メチルスルホニル)エチル]アミノ]メチル]フラン-2-イル]キナゾリン

N-[3-クロロ-4-[(3-フルオロベンジル)オキシ]フェニル]-6-[5-[[[2-(メチルスルホニル)エチル]アミノ]メチル]フラン-2-イル]キナゾリン-4-アミン

ラパチニブ物理性質

融点	144-146oC
沸点	750.7±60.0 °C(Predicted)
比重(密度)	1.381±0.06 g/cm3(Predicted)
貯蔵温度	2-8°C(protect from light)
溶解性	DMSO に可溶 (200 mg/ml まで)
外見	個体
酸解離定数(Pka)	6.34±0.19(Predicted)
色	黄色
安定性：	-20°C の DMSO 溶液で最大 1 か月間保存できます。
InChIKey	BCFGMOOMADDAQU-UHFFFAOYSA-N
SMILES	N1=C2C(C=C(C3=CC=C(CNCCS(C)(=O)=O)O3)C=C2)=C(NC2=CC=C(OCC3=CC=CC(F)=C3)C(Cl)=C2)N=C1
CAS データベース	231277-92-2(CAS DataBase Reference)

安全性情報

HSコード	29349990
有毒物質データの	231277-92-2(Hazardous Substances Data)

危険有害性情報のコード(GHS)

ラパチニブ化学特性,用途語,生産方法

効能
抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬
説明
Lapatinib, a new member of the 4-anilinoquinazoline class of RTK inhibitors (RTKIs), was launched as an oral treatment for breast cancer. Lapatinib has dual affinity for EGFR and HER2 tyrosine kinases. It is indicated in combination with capecitabine for treating patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and trastuzumab. Previously marketed drugs from the 4-anilinoquinazoline class include erlotinib (Tarceva) and gefitinib (Iressa^TM), both of which are indicated for treating non-small-cell lung cancer (NSCLC). As with erlotinib and gefitinib, To Market, To Market 2007 475 lapatinib is an ATP-competitive kinase inhibitor. It inhibits the tyrosine kinase activity EGFR and HER-2 with apparent Ki values of 3 and 13 nM, respectively, and has slow off-rate kinetics (t1/2X300 min).
In addition, dividing the daily dose of lapatinib results in approximately 2-fold higher exposure at steady state compared to the same total dose administered once daily.
The chemical synthesis of lapatinib entails the condensation of 4-chloro-6-iodoquinazoline and 3-chloro-4-(3-fluorobenzyloxy)aniline to produce a diaryl amine intermediate followed by Stille coupling of the iodo group with 5-dioxolanyl-2-(tributylstannyl)furan and subsequent acid hydrolysis of the cyclic ketal to the corresponding aldehyde. Finally, reductive amination of the aldehyde intermediate with 2-(methanesulfonyl) ethylamine in the presence of sodium triacetoxyborohydride produces lapatinib. .
一般的な説明
Class: receptor tyrosine kinase
Treatment: HER2-positive breast cancer
Elimination half-life = 24 h
Protein binding = 99%

ラパチニブ上流と下流の製品情報

ラパチニブ生産企業

ラパチニブスペクトルデータ(MS)

231277-92-2, ラパチニブキーワード

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ラパチニブ

危険有害性情報のコード(GHS)

ラパチニブ 化学特性,用途語,生産方法

ラパチニブ 上流と下流の製品情報

ラパチニブ 生産企業

ラパチニブ スペクトルデータ(MS)

231277-92-2, ラパチニブ キーワード

ラパチニブ化学特性,用途語,生産方法

ラパチニブ上流と下流の製品情報

ラパチニブ生産企業

ラパチニブスペクトルデータ(MS)

231277-92-2, ラパチニブキーワード