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WZ4002是一种新型的，突变选择性EGFR抑制剂，作用于EGFR(L858R)/(T790M)，在BaF3细胞系中IC50为2 nM/8 nM；对ERBB2磷酸化(T798I)没有抑制作用。
靶点信息
| EGFR (L858R) (BaF3 cells) | EGFR (L858R/T790M) (BaF3 cells) | |||
| 2 nM | 8 nM |
| In vitro (25°C) | DMSO | 12 mg/mL (24.28 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 28 mg/mL | |
|
* <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. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 20.2 mL | 101.01 mL | 202.02 mL |
| 0.5 mM | 4.04 mL | 20.2 mL | 40.4 mL |
| 1 mM | 2.02 mL | 10.1 mL | 20.2 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
*The above data is based on the productmolecular weight 495.0. 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.
| 目录号 | A10991 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 495.0 |
| Formula | C25H27ClN6O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 1213269-23-8 |
| SMILES | CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)OC4=CC=CC(=C4)NC(=O)C=C)Cl)OC |
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