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Tucatinib hemiethanolate

Catalog No. T36648 CAS 1429755-56-5

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

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Tucatinib hemiethanolate Chemical Structure

Tucatinib hemiethanolate, CAS 1429755-56-5

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2 mg	5 days	$ 30.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
Targets&IC50	HER2:8 nM (IC50)
In vitro	Tucatinib hemiethanolate exhibits nanomolar potency against the purified HER2 enzyme, displaying approximately 500-fold greater selectivity for HER2 over EGFR in cell-based assays. This compound specifically targets and inhibits the receptor tyrosine kinase HER2, with minimal activity towards EGFR, thus potentially avoiding EGFR-related toxicities. It effectively hinders both proliferation and phosphorylation of HER2 and its downstream effector Akt in HER2-overexpressing cell lines. Conversely, in cell lines with elevated EGFR expression, tucatinib only modestly affects phosphorylation and proliferation, underscoring its promise in selectively disrupting HER2 signaling pathways[1].
In vivo	Tucatinib hemiethanolate (ONT-380 hemiethanolate, 200 mg/kg/d) improves survival when administered at the maximum-tolerated dose[1] and, along with its active metabolite, significantly lowers brain pErbB2 levels by 80%[2]. This compound (ARRY-380 hemiethanolate) also exhibits notable tumor growth inhibition (TGI)—50% at 50 mg/kg/d and up to 96% at 100 mg/kg/d, resulting in numerous partial regressions (over 50% reduction from baseline size) in 9 out of 12 animals at the higher dosage. Moreover, when combined with trastuzumab at 50 mg/kg/d, it achieves a 98% TGI, with complete tumor regressions observed in 9 out of 12 animals and two showing partial regressions[3].

Molecular Weight	1007.133
Formula	C54H54N16O5
CAS No.	1429755-56-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (248.23 mM), Sonication is recommended.

References and Literature

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. 3. P. Lee, et al. In Vivo Activity of ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2 in Combination with RP-56976. Cancer Research.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Tucatinib hemiethanolate 1429755-56-5 Tucatinib Tucatinib Hemiethanolate inhibitor inhibit

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