TAS0728

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Chemical Structure| 2088323-16-2 同义名 : TPC 107
CAS号 : 2088323-16-2
货号 : A1176741
分子式 : C26H32N8O3
纯度 : 99%+
分子量 : 504.58
MDL号 : MFCD31813813
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(237.82 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 TAS0728 is a potent, selective, orally active, irreversible and covalently bound HER2 inhibitor with an IC50 of 13 nM. The IC50s of TAS0728 against BMX, HER4, BLK, EGFR, JAK3, SLK, and LOK were 4.9, 8.5, 31, 65, 33, 25, and 86 nM respectively. In addition, TAS0728 inhibited HER2, HER4, BLK, EGFR, JAK3 and LOK with an IC50 of 4.9, 8.5, 31, 65, 33, 25, and 86 nM. TAS0728 potently and consistently inhibited the phosphorylation of HER2, HER3 and downstream effectors. In the HER2-amplified SK-BR-3/AU565/BT-474/NCI-N87/Calu-3 cell line, TAS0728 showed antiproliferative effects with GI50 values of 5.0/5.1/3.6/1.6/6.9 nM, respectively[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.91mL

1.98mL

0.99mL

19.82mL

3.96mL

1.98mL
参考文献

[1]Irie H, et al. TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models. Molecular cancer therapeutics. 2019;18(4):733-42. Epub 2019/02/23.