Tucatinib|937263-43-9|(Irbinitinib; ARRY-380; ONT-380)-陌孚医药/Medlife

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Tucatinib (Synonyms: Irbinitinib; ARRY-380; ONT-380)

目录号: PL04585 纯度: ≥99%

CAS No. :937263-43-9

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中文名称	Tucatinib
中文别名	N6-(4,5-二氢-4,4-二甲基-2-噁唑)-N4-[3-甲基-4-([1,2,4]噻唑并[1,5-a]吡啶-7-基氧基)苯基]-4,6-喹唑啉二胺;埃克替尼
英文名称	Tucatinib
英文别名	N6-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine;ARRY-380;Irbinitinib;Irbinitinib (ARRY-380);N6-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolined...;ONT-380;ARRY 380;ONT 380;Tucatinib;6-DIAMINE;234248D0HH;Tucatinib [USAN:INN];Tucatinib (USAN/INN);N6-(4,4-Dimethyl-4,5-dihydrooxazol-2-yl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine;GTPL9922;SDEAXTCZPQIFQM-UHFFF;N6-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine (ACI);Tukysa
Cas No.	937263-43-9
分子式	C₂₆H₂₄N₈O₂
分子量	480.52
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Tucatinib (Irbinitinib) 是有效，具有口服活性的、选择性的 HER2 抑制剂，IC₅₀ 为8 nM。

生物活性

Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC 50 of 8 nM.

性状

Solid

IC50 & Target[1][2]

HER2

体外研究(In Vitro)

Tucatinib has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR.
Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that Tucatinib may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Tucatinib (ONT-380, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose.
Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%).
Tucatinib (ARRY-380) demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Moulder-Thompson S, et al. Phase 1 Study of ONT-380, a HER2 Inhibitor, in Patients with HER2 Advanced Solid Tumors, with an Expansion Cohort in HER2+ Metastatic Breast Cancer (MBC). Clin Cancer Res. 2017 Jan 4. pii: clincanres.1496.2016.
[2]. Abstract: In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 852. doi:1538-7445.AM2012-852

溶解度数据	In Vitro: DMSO : 41.67 mg/mL (86.72 mM; ultrasonic and warming and heat to 60°C)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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