Theliatinib (HMPL-309)
产品编号: DC10764
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应用领域
Theliatinib (HMPL-309) 是一种有效、ATP 竞争性、口服活性和高度选择性的 EGFR 抑制剂，Ki 为 0.05 nM，IC50 为 3 nM。Theliatinib 对 EGFR T790M/L858R 突变体的 IC50 值为 22 nM。Theliatinib 对 EGFR 的选择性是其他激酶的 50 倍以上。抗肿瘤活性。
| Cas No.: |
1353644-70-8 |
| 名称: |
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| 别名: |
HMPL-309,HMPL 309，HMPL309 |
| SMILES: |
C1=CC(NC2C3C=C(NC(=O)N4C[C@@]([H])5N(C)CC[C@]5([H])C4)C(OC)=CC3=NC=N2)=CC(C#C)=C1 |
| 分子式: |
C25H28N6O2 |
| 分子量: |
444.23 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vitro: |
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| References: |
Theliatinib (HMPL-309) is a novel small molecule, epidermal growth factor receptor tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities. Theliatinib is being developed as an oral formulation for the treatment of solid tumors like non-small cell lung cancer.Theliatinib pre-clinical studies were conducted in China. In vitro studies suggest that Theliatinib is a potent EGFR kinase inhibitor with good kinase selectivity and in vivo data demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as A-431, Bcap-37 and Fadu. Non-clinical safety studies have indicated that Theliatinib is generally well tolerated in animals. |
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MSDS
| TITLE |
DOWNLOAD |
| MSDS_511_DC10764_1353644-70-8 |
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COA
| LOT NO. |
DOWNLOAD |
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