TAS0728
Cat. No.：YN340073
CAS No. ：2088323-16-2
| 产品名称: | TAS0728 |
| CAS No.: | 2088323-16-2 |
| Chemical Name: | 4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]-2,3-dimethylphenyl]-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide |
| Synonyms: | TAS0728|TAS-0728;TAS 0728 |
| 分子量: | 504.58 |
| 分子式: | C₂₆H₃₂N₈O₃ |
| SMILES: | NC1=C2C(N([C@H]3CN(C(C=C)=O)CCC3)N=C2C(NC4=CC=C(CC(N(C)C)=O)C(C)=C4C)=O)=NC=N1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | TAS0728 是一种有效、选择性、可口服、不可逆、共价结合的HER2抑制剂，与HER2的 C805 位点共价结合，抑制其活性，IC50值为 13 nM。TAS0728 对 BMX，HER4，BLK，EGFR，JAK3，SLK，LOK 和 人 HER2 的IC50值分别为 4.9，8.5，31，65，33，25，86 和 36 nM。TAS0728 同时可抑制 HER2，HER3 及其下游效应蛋白的磷酸化。具有抗肿瘤活性。 |
| IC50和靶点: | [{name:"HER4:8.5 nM (IC50)"},{name: "HER2:13 nM (IC50)"},{name: "EGFR:65 nM (IC50)"},{name: "BMX:4.9 nM (IC50)"},{name: "BLK:31 nM (IC50)"},{name: "JAK3:33 nM (IC50)"},{name: "SLK:25 nM (IC50)"},{name: "LOK:86 nM (IC50)"}] |
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Irie, H., Ito, K., Fujioka, Y., et al.TAS0728, a covalent-binding, HER2-selective kinase inhibitor shows potent antitumor activity in preclinical modelsMol. Cancer Ther.18(4),733-742(2019)
