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Erlotinib是一种表皮生长因子受体抑制剂(EGFR抑制剂),抑制纯化 EGFR 激酶的 IC50 为2 nM。厄洛替尼以可逆方式与受体的三磷酸腺苷(ATP)结合位点结合。为了传递信号,需要将两个EGFR分子聚在一起形成同型二聚体。然后,这些分子利用ATP分子在酪氨酸残基上彼此进行反磷酸化,从而产生磷酸酪氨酸残基,将磷酸酪氨酸结合蛋白募集到EGFR,从而组装将信号级联转导至细胞核或激活其他细胞生化过程的蛋白复合物。当厄洛替尼与EGFR结合时,就不可能在EGFR中形成磷酸酪氨酸残基,并且不会引发信号级联。
In vitro (25°C) | DMSO | 68 mg/mL (172.83 mM) | |
Water | Insoluble | ||
Ethanol | Warmed: 13 mg/mL | ||
In vivo | 5% DMSO+30% PEG 300+5% Tween 80+ddH2O | 5 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 | 25.42 mL | 127.08 mL | 254.17 mL |
0.5 mM | 5.08 mL | 25.42 mL | 50.83 mL |
1 mM | 2.54 mL | 12.71 mL | 25.42 mL |
5 mM | 0.51 mL | 2.54 mL | 5.08 mL |
*The above data is based on the productmolecular weight 393.443. 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 | A11416 |
---|---|
作用机制 | Inhibitor (抑制剂) |
M. Wt | 393.443 |
Formula | C22H23N3O4? |
Purity | >99% |
Storage | Store lyophilized at -20ºC, keep desiccated. |
CAS No. | 183321-74-6 |
Synonyms | CP-358,774, CP-358774, CP358774, OSI-774, OSI 774, OSI774, Erlotinib free base. |
SMILES | COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC |
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