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Tucatinib hemiethanolate

Catalog No. T36648Cas No. 1429755-56-5
Alias ONT-380 hemiethanolate, Irbinitinib hemiethanolate, ARRY-380 hemiethanolate

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

Tucatinib hemiethanolate

Tucatinib hemiethanolate

Purity: 99.76%
Catalog No. T36648Alias ONT-380 hemiethanolate, Irbinitinib hemiethanolate, ARRY-380 hemiethanolateCas No. 1429755-56-5
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.
Pack SizePriceAvailabilityQuantity
5 mg$40In Stock
10 mg$61In Stock
25 mg$98In Stock
50 mg$139In Stock
100 mg$198In Stock
1 mL x 10 mM (in DMSO)$44In Stock
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Purity:99.76%
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Product Introduction

Bioactivity
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 hemiglycolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 over EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 but not EGFR[1].
In vivo
Tucatinib hemiethanolate (ONT-380 hemiethanolate, 200 mg/kg/d) improves survival at maximum-tolerated dose[1] and reduces brain pErbB2 levels by 80%[2]. This compound (ARRY-380 hemiethanolate) shows significant tumor growth inhibition (TGI)—50% at 50 mg/kg/d and up to 96% at 100 mg/kg/d, with over 50% reduction in baseline tumor size in 9 out of 12 animals at the higher dosage. When combined with trastuzumab at 50 mg/kg/d, it achieves 98% TGI, with complete regressions in 9 out of 12 animals and partial regressions in two[3].
AliasONT-380 hemiethanolate, Irbinitinib hemiethanolate, ARRY-380 hemiethanolate
Chemical Properties
Molecular Weight1007.11
FormulaC54H54N16O5
Cas No.1429755-56-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (248.23 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.9929 mL4.9647 mL9.9294 mL49.6470 mL
5 mM0.1986 mL0.9929 mL1.9859 mL9.9294 mL
10 mM0.0993 mL0.4965 mL0.9929 mL4.9647 mL
20 mM0.0496 mL0.2482 mL0.4965 mL2.4824 mL
50 mM0.0199 mL0.0993 mL0.1986 mL0.9929 mL
100 mM0.0099 mL0.0496 mL0.0993 mL0.4965 mL

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