| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (248.23 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to off-white | [InChIKey]
WCRUOHQGIAPBOG-UHFFFAOYSA-N | [SMILES]
C(O)C.N(C1C=CC(OC2C=CN3N=CN=C3C=2)=C(C)C=1)C1=NC=NC2C=CC(NC3OCC(C)(C)N=3)=CC1=2 |
| Hazard Information | Back Directory | [Uses]
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. | [in vivo]
Tucatinib hemiethanolate (ONT-380 hemiethanolate, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose[1].
Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%)[2].
Tucatinib (ARRY-380) hemiethanolate 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[3].
| Animal Model: | Female nude mice[3]. | | Dosage: | 200 mg/kg/d. | | Administration: | PO, daily. | | Result: | Exhibited anti-tumor activity and benefited survival. |
| [storage]
Store at -20°C | [References]
[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. DOI:10.1158/1078-0432.CCR-16-1496
[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. |
|
|