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1365267-27-1

中文名稱 恩沙替尼(X 396)
英文名稱 X-376
CAS 1365267-27-1
分子式 C25H25Cl2FN6O3
分子量 547.409
MOL 文件 1365267-27-1.mol
更新日期 2024/12/16 09:27:32
1365267-27-1 結(jié)構(gòu)式 1365267-27-1 結(jié)構(gòu)式

基本信息

中文別名
恩沙替尼
恩沙替尼(X-376)
恩沙替尼(X 396)
ALK抑制劑(ENSARTINIB)
英文別名
X-396
X-376
CS-1720
Ensartinib
(R)-6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-N-(4-(4-methylpiperazine-1-carbonyl)phenyl)pyridazine-3-carboxamide
6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide
6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-3-pyridazinecarboxamide
3-Pyridazinecarboxamide, 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)695.1±55.0 °C(Predicted)
密度1.428±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度Ethanol:13.0(Max Conc. mg/mL);23.75(Max Conc. mM)
酸度系數(shù)(pKa)10.70±0.70(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302

常見問題列表

二代ALK抑制劑
二代ALK抑制劑恩沙替尼(X-396)全面優(yōu)于第一代克唑替尼,2016年6月開始全球多中心3期臨床,2017年6月獲批多中心國內(nèi)3期臨床批件,均為一線用藥,預(yù)計2019~2021年將上市銷售。預(yù)計全球銷售額5億美元級別,其中海外3億美元,國內(nèi)12億元。此外,X-396還于2017年12月在美國啟動“ALK陽性晚期惡性黑色素瘤”2期臨床研究,是全球首個ALK抑制劑治療黑色素瘤的臨床研究,有望以“孤兒藥”獲批上市。市場空間8億美元,以滲透率40%計算,銷售峰值為3.2億美元??傮w銷售峰值在50億元左右。
市場情況
恩沙替尼處于一線治療 III 期臨床,療效有望看齊艾樂替尼,將和艾樂替尼、 Brigatinib 共同競爭國際市場;恩沙替尼有望復(fù)制??颂婺岬某晒Α?恩沙替尼國內(nèi)有望以優(yōu)異的 II 期臨床數(shù)據(jù)直接申請上市,復(fù)制??颂婺岬某晒?,國內(nèi)峰值銷售有望超過 20 億元。
可能的副作用

恩沙替尼治療較常見的副作用包括皮疹、瘙癢、水腫、貧血等,大多數(shù)為1-2級,程度輕微,發(fā)生率最高的3級或以上明顯副作用為皮疹(6%)和顏面部水腫(4%)。恩沙替尼治療過程中較常見的實(shí)驗(yàn)室檢查結(jié)果異常,包括肝酶兩項(xiàng)、γ-谷氨酰轉(zhuǎn)肽酶、堿性磷酸酶、血清淀粉酶和血肌酐升高。

生物活性
X-376是ALK抑制劑,對治療非小細(xì)胞性肺癌有潛在療效。
靶點(diǎn)
TargetValue
ALK
()
體外研究

The ability of X-376 to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. X-376 is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC 50 : 77 nM). X-376 is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC 50 : 57 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC 50 : 32 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC 50 s of 142 nM, 150 nM, 15.137 μM and 3.062 μM, respectively.

體內(nèi)研究

The effects of X-376 in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that X-376 shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with X-376 at 50 mg/kg bid. X-376 significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, X-376 appears well-tolerated in vivo. Mouse weight is unaffected by X-376 treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of X-376, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of X-376 at 25, 50, 100 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 50 mg/kg for X-376. At NST levels, X-376 achieves an AUC of 41 μM×hr and a C max of 5.04 μM.

恩沙替尼價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-16590恩沙替尼
X-376
1365267-27-12mg890元
2024/11/08HY-16590恩沙替尼
X-376
1365267-27-15mg1700元
2024/11/08HY-16590恩沙替尼
X-376
1365267-27-110mM * 1mLin DMSO2047元
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