Tucatinib (Irbinitinib, ONT-380, ARRY-380)

Chemical Structure : Tucatinib

CAS No.: 937263-43-9

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货号: 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.

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10 mg	￥780	In stock
50 mg	￥1780	In stock
100 mg	￥2680	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	480.53
分子式	C26H24N8O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.