라파티닙
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라파티닙 속성
- 녹는점
- 144-146oC
- 끓는 점
- 750.7±60.0 °C(Predicted)
- 밀도
- 1.381±0.06 g/cm3(Predicted)
- 저장 조건
- 2-8°C(protect from light)
- 용해도
- DMSO에 용해됨(최대 200mg/ml)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 산도 계수 (pKa)
- 6.34±0.19(Predicted)
- 색상
- 노란색
- 안정성
- 제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
- 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 데이터베이스
- 231277-92-2(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
| HS 번호 | 29349990 | ||
|---|---|---|---|
| 유해 물질 데이터 | 231277-92-2(Hazardous Substances Data) |
라파티닙 C화학적 특성, 용도, 생산
개요
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 (IressaTM), 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. .
일반 설명
Class: receptor tyrosine kinaseTreatment: HER2-positive breast cancer
Elimination half-life = 24 h
Protein binding = 99%
라파티닙 준비 용품 및 원자재
원자재
5-[4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl]-2-furaldehyde
Lapatinib ditosylate
1227853-06-6
2-아미노에틸메틸술폰
준비 용품
라파티닙 공급 업체
글로벌( 524)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| ZHEJIANG ESTCHEM CO.,LTD | 15957180504 |
sales@zjestchem.com | China | 193 | 58 |
| SHANDONG BOYUAN PHARMACEUTICAL CO., LTD. | +86-0531-69954981 +8615666777973 |
dwyane.wang@boyuanpharm.com | China | 211 | 58 |
| Hebei Yanxi Chemical Co., Ltd. | +8617531190177 |
peter@yan-xi.com | China | 6011 | 58 |
| Hebei Guanlang Biotechnology Co,.LTD | +86-19930503253; +8619930503252 |
daisy@crovellbio.com | China | 5957 | 58 |
| Henan Bao Enluo International TradeCo.，LTD | +86-17331933971 +86-17331933971 |
deasea125996@gmail.com | China | 2503 | 58 |
| Sigma Audley | +86-18336680971 +86-18126314766 |
nova@sh-teruiop.com | China | 525 | 58 |
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29797 | 60 |
| Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21688 | 55 |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9341 | 55 |