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エルロチニブ塩酸塩 (TARCEVA)

エルロチニブ塩酸塩 (TARCEVA) 化学構造式
183319-69-9
CAS番号.
183319-69-9
化学名:
エルロチニブ塩酸塩 (TARCEVA)
别名:
エルロチニブ塩酸塩 (TARCEVA);エルロチニブ塩酸塩;TARCEVA (エルロチニブ塩酸塩);エルロニチブ塩酸塩;エルロチニブ塩酸塩 (JAN)
英語化学名:
Erlotinib hydrochloride
英語别名:
RG-1415;Tarceva;OSI 774;CP 358774;NSC718781;RO-0508231;CP-358774-01;ERLOTINIB HCL;Erlotonid HCl;NSC 718781) HCl
CBNumber:
CB2285915
化学式:
C22H24ClN3O4
分子量:
429.9
MOL File:
183319-69-9.mol

エルロチニブ塩酸塩 (TARCEVA) 物理性質

融点 :
223-225°C
貯蔵温度 :
-20°C Freezer
酸解離定数(Pka):
pKa (25°): 5.42
外見 :
Yellow powder.
CAS データベース:
183319-69-9(CAS DataBase Reference)

安全性情報

Sフレーズ  24/25
HSコード  29335990

エルロチニブ塩酸塩 (TARCEVA) 価格 もっと(17)

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
富士フイルム和光純薬株式会社(wako) W01COBST-7799
Erlotinib, HCl
183319-69-9 5g ¥14400 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBST-7799
Erlotinib, HCl
183319-69-9 1g ¥4300 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01LKTE6846 エルロチニブ塩酸塩
Erlotinib Hydrochloride
183319-69-9 10mg ¥6400 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01W0105-0911 エルロチニブ塩酸塩 98.0+% (HPLC)
Erlotinib Hydrochloride 98.0+% (HPLC)
183319-69-9 100mg ¥8000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01LKTE6846 エルロチニブ塩酸塩
Erlotinib Hydrochloride
183319-69-9 25mg ¥8300 2018-12-26 購入

エルロチニブ塩酸塩 (TARCEVA) 化学特性,用途語,生産方法

外観

白色~うすい褐色、結晶性粉末~粉末

溶解性

ジメチルスルホキシドに溶け、アセトン及び水にほとんど溶けない。

用途

上皮成長因子受容体(EGFR) チロシンキナーゼの阻害剤です。EGFR 遺伝 子変異による、腫瘍細胞の増殖を抑制する作 用を示します。

効能

抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬

商品名

タルセバ (中外製薬); タルセバ (中外製薬)

説明

Erlotinib, launched as once daily oral treatment for patients with non-small-cell lung cancer (NSCLC), is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, and it is the second small-molecule drug to be marketed with this mechanism of action. Both erlotinib and its predecessor, gefitinib, are members of the anilinoquinazoline class of tyrosine kinase inhibitors. They compete with the binding of ATP to the intracellular tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and blocking downstream signal transduction. Erlotinib is prepared by the condensation of 3-ethynylaniline with 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline, which is a key intermediate obtained in five synthetic steps starting from ethyl 3,4- dihydroxybenzoate. In vitro, Erlotinib inhibits purified human EGFR tyrosine kinase with an IC50 of 2 nM and blocks EGFR autophosphorylation in cellular assays with an IC50 of 20nM. Treatment of human colon cancer cells with erlotinib was associated with growth inhibition, G1 cell cycle arrest, and apoptosis. Oral administration of erlotinib in athymic mice produced potent antitumor effects with an ED50 of 9.2 mg/kg/day for HN5 head and neck xenografts and 14 mg/ kg/day for A431 epidermoid xenografts. The absorption of Erlotinib following oral dosing is approximately 60%. Food greatly enhances the absorption allowing for almost 100% bioavailability of the dose. The time to reach peak plasma levels of the drug is about 4 hours, and the half-life is approximately 36 hours. Steady-state drug levels are reached in 7 to 8 days. Erlotinib has high protein binding (93%) and has an apparent volume of distribution of 232 L. It is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2 and CYP1A1. The drug is mainly excreted in the feces with less than 9% of the dose found in the urine. Erlotinib is labeled for the treatment of patients with locally advanced or metastatic NSCLC who have failed one or more previous chemotherapy regimens. The recommended dosage is 150 mg daily until disease progression is detected. In a randomized, double blind, placebo-controlled trial involving 731 patients, 150 mg/day oral dose of erlotinib resulted in a median overall survival of 6.7 months compared with 4.7 months in the placebo group (p<0.001). Progression-free survival was 9.9 weeks and 7.9 weeks in the erlotinib and placebo groups, respectively (p<0.001). Survival at one year was 31.2% in the erlotinib group versus 21.5% in the placebo group. The use of erlotinib showed greater benefit in patients with EGFR positive tumors and in those who never smoked. The most common adverse events reported in clinical trials were rash (9%) and diarrhea (6%). Elevations in liver function tests were also seen; however, these effects were mainly transient or associated with liver metastases. As previously noted for gefitinib, erlotinib is also shown to lack any clinical benefit in concurrent administration with platinum-based chemotherapy.

化学的特性

Off-White Solid

Originator

Pfizer (US)

使用

Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor. Antineoplastic

使用

Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.

使用

Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Phase 3.

定義

ChEBI: A quinazoline hydrochloride compound having a (3-ethynylphenyl)amino group at the 4-position and two 2-methoxyethoxy groups at the 6- and 7-positions.

brand name

Tarceva (OSI).

一般的な説明

Erlotinib is available as 25-, 100-, and 150-mg tablets fororal administration and is used after failure of first-linetherapy in metastatic NSCLC and as first-line therapy incombination with gemcitabine in the treatment of metastaticpancreatic cancer, and in treating malignant gliomas.The structural similarity to gefitnib imparts similar pharmacokineticbehavior with bioavailability of 60% and proteinbinding of 93%. The agent is extensively metabolizedprimarily by CYP3A4. Three major metabolic pathwayshave been identified, involving oxidative-O-demethylationof the side chains followed by further oxidation to give thecarboxlic acids, oxidation of the acetylene functionalityto give a carboxylic acid, and aromatic hydroxylation ofthe phenyl ring para to the electron-donating nitrogen. Themetabolites are primarily eliminated in the feces, and theterminal half-life is 36 hours.The major toxicities seenwith the agent are dose-limiting skin rash and diarrhea.Other common adverse effects include shortness of breath,fatigue, and nausea.

生物活性

Erlotinib inhibits EGFR tyrosine kinase auto-phosphorylation. Studies in cell lines and enzyme assays have shown that erlotinib inhibits EGFR at concentrations significantly lower than those needed to inhibit c-src and v-abl. It has an IC50 of 2 nM against EGFR. It is >1000-fold more sensitive for EGFR than for c-Src or v-Abl.

エルロチニブ塩酸塩 (TARCEVA) 上流と下流の製品情報

原材料

準備製品


エルロチニブ塩酸塩 (TARCEVA) 生産企業

Global( 395)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 886 50
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3194 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21745 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32447 55
Hangzhou FandaChem Co.,Ltd.
0086 158 5814 5714 (Mobile; WhatsApp; Telegram)
+86-571-56059825 fandachem@gmail.com CHINA 2839 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 661 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24192 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 209 58

183319-69-9(エルロチニブ塩酸塩 (TARCEVA))キーワード:


  • 183319-69-9
  • Erlotinib HCl (OSI-744)
  • Erlotinib hydrochloride, 98.5%
  • Tarceva, CP-358774
  • Erlotinib Hydrochloride WS
  • NSC 718781) HCl
  • Erlotinib hydrochloride N-(3-Ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine hydrochloride
  • Erlotinib HCl, >=99%
  • CP-358774-01
  • RG-1415
  • RO-0508231
  • Erlotinib impurity O
  • Erlotinib (OSI-744) HCl
  • Erlotinib Hcl(CP-358)
  • ERLOTINIB HCL
  • 6,7-Bis(2-methoxyethoxy)-4-(3-
  • Erlotinib hydrochlroide
  • ERLOTINIB HCL SALT
  • ERLOTINIB HCL SALT :TARCEVA
  • Erlotinib, Hydrochloride Salt
  • N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, Hydrochloride Salt, OSI 774, Tarceva
  • N-(3-Ethynylphenyl)-6,7-bis-(2-methoxyethoxy)-quinazolin-4-amine
  • [6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4yl]-(3-ethynyl-phenyl)-amine
  • Tarceva Hydrochloride See E625000
  • Erlotinib HCl(TINIBS)
  • 6,7-Bis(2-methoxyethoxy)-4-(3-ethynylanilino)quinazoline hydrochloride
  • Erlotinib hydrochloride
  • N-(3-Ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine hydrochloride
  • Tarceva
  • erlotinib hydorchloride
  • 6,7-BIS(2-METHOXYETHOXY)-4-(3-ETHYNYLANILINO)QUINAZOLINE HCL
  • エルロチニブ塩酸塩 (TARCEVA)
  • エルロチニブ塩酸塩
  • TARCEVA (エルロチニブ塩酸塩)
  • エルロニチブ塩酸塩
  • エルロチニブ塩酸塩 (JAN)
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