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Chemical Structure : Tucatinib
CAS No.: 937263-43-9
Catalog No.: PC-38023Not For Human Use, Lab Use Only.
Tucatinib (Irbinitinib, ONT-380, ARRY-380) is a potent, selective, reversible and ATP-competitive inhibitor of ErbB-2 (HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $218 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | $698 | In stock | |
| 250 mg | Get quote |
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Tucatinib (Irbinitinib, ONT-380, ARRY-380) is a potent, selective, reversible and ATP-competitive inhibitor of ErbB-2 (HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively.
Tucatinib displays 500-fold selective for HER2 versus EGFR in cell-based assays.
Tucatinib inhibits the phosphorylation of HER2 in a L755S mutant MCF-10A cell line and inhibits the growth of 3 L755S mutant tumor models derived from colorectal, gastric and non-small cell lung cancer.
Tucatinib also potently inhibits the phosphorylation of HER2 in a V777L mutant MCF-10A cell line, and in a colorectal PDX model containing a V777L mutation, tucatinib alone or in combination with trastuzumab induces tumor regressions.
Tucatinib inhibits HER2 phosphorylation, but not EGFR phosphorylation, and inhibits the phosphorylation of HER2, HER3, Erk1/2, MEK1 and AKT in the G776V_G/C HER2 mutant NCI-H1781 cell line.
| M.Wt | 480.53 | |
| Formula | C26H24N8O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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 |
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1. Moulder SL, et al. Clin Cancer Res. 2017 Jul 15;23(14):3529-3536.
2. Murthy RK, et al. N Engl J Med. 2020 Feb 13;382(7):597-609.
3. Kulukian A, et al. Mol Cancer Ther. 2020 Apr;19(4):976-987.
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