Erlotinib

Catalog No. A11416

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。

Product Citations

Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
Manabe A, .et al. Upregulation of transient receptor potential melastatin 6 channel expression by rosiglitazone and all-trans-retinoic acid in erlotinib-treated renal tubular epithelial cells, J Cell Physiol, 2018, Nov 21 PMID: 30461012
Yui Takashina, .et al. Sodium Citrate Increases Expression and Flux of Mg2+ Transport Carriers Mediated by Activation of MEK/ERK/c-Fos Pathway in Renal Tubular Epithelial Cells, Nutrients, 2018, Oct; 10(10): 1345 PMID: 30241394
Furukawa C, .et al. Up-Regulation of Transient Receptor Potential Melastatin 6 Channel Expression by Tumor Necrosis Factor-α in the Presence of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, J Cell Physiol, 2017, Oct;232(10):2841-2850 PMID: 27925186
Xiaoyu Yang, .et al. Knockdown delta-5-desaturase promotes the formation of a novel free radical byproduct from COX-catalyzed ω-6 peroxidation to induce apoptosis and sensitize pancreatic cancer cells to chemotherapy drugs, Free Radic Biol Med, 2016, Aug; 97: 342-350 PMID: 27368132

Technical details

Catalog Num	A11416
M. Wt	393.443
Formula	C22H23N3O4?
Purity	>98%
Storage	at -20°C 3 years Powder
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

Biological Activity

Solubility *

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.

Preparing Stock Solutions

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.