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Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $40 | In Stock | |
10 mg | $61 | In Stock | |
25 mg | $98 | In Stock | |
50 mg | $139 | In Stock | |
100 mg | $198 | In Stock | |
1 mL x 10 mM (in DMSO) | $44 | In Stock |
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]. |
Alias | ONT-380 hemiethanolate, Irbinitinib hemiethanolate, ARRY-380 hemiethanolate |
Molecular Weight | 1007.11 |
Formula | C54H54N16O5 |
Cas No. | 1429755-56-5 |
Smiles | CCO.Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1.Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1 |
Relative Density. | no data available |
Storage | Powder: -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
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