生物活性
TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型，ATP竞争性和选择性抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,具有潜在的抗肿瘤活性。
靶点信息
| JAK2 (Cell-free assay) | JAK2 (V617F) (Cell-free assay) | FLT3 (Cell-free assay) | RET (Cell-free assay) | |
| 3 nM | 3 nM | 15 nM | 48 nM | |
化学数据
| 目录号 | A11082 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 524.7 |
| Formula | C27H36N6O3S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 936091-26-8 |
| Synonyms | SAR302503,TG101348,TG101348 |
| SMILES | CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4 |
溶解度
| In vitro | DMSO | 90 mg/mL (171.53 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 19.06 mL | 95.29 mL | 190.59 mL |
| 0.5 mM | 3.81 mL | 19.06 mL | 38.12 mL |
| 1 mM | 1.91 mL | 9.53 mL | 19.06 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.81 mL |
*The above data is based on the productmolecular weight 524.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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