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| | Epertinib hydrochloride Basic information |
| Product Name: | Epertinib hydrochloride | | Synonyms: | Epertinib hydrochloride;S-222611 HCL;S-22611 hydrochloride;Epertinib HCL;inhibit,Epidermal growth factor receptor,EGFR,S22611,Epertinib,Epertinib hydrochloride,ErbB-1,HER1,S 22611,S-22611,Inhibitor;Epertinib hydrochloride, 10 mM in DMSO;(R,Z)-1-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)but-2-yn-1-one O-morpholin-3-ylmethyl oxime hydrochloride | | CAS: | 2071195-74-7 | | MF: | C30H28Cl2FN5O3 | | MW: | 596.48 | | EINECS: | | | Product Categories: | | | Mol File: | 2071195-74-7.mol |  |
| | Epertinib hydrochloride Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 125 mg/mL (209.56 mM) | | form | Solid | | color | Light yellow to yellow |
| | Epertinib hydrochloride Usage And Synthesis |
| Uses | Epertinib Hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4. | | in vivo | Epertinib hydrochloride (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity[1].
Epertinib hydrochloride (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume[1].
Epertinib hydrochloride (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner[2]. | Animal Model: | Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1] | | Dosage: | 12.5, 25, 50, 100 mg/kg | | Administration: | Orally, once daily for 28 days | | Result: | Showed antitumor activity in the mammary fat pad implantation model using both cell lines and the ED50 values were comparable (24.1mg/kg and 26.5mg/kg for MDA-MB-361 and BR2 (MDA-MB-361-luc-BR2), respectively). |
| Animal Model: | Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1] | | Dosage: | 50 mg/kg | | Administration: | Orally, once daily for 30 days | | Result: | Significantly reduced the brain tumor volume, indicating that epertinib could have potent antitumor activity in brain metastasis even in the presence of an intact BTB (blood-tumor barrier). |
| Animal Model: | Nude mice (BALB/cAJcl-nu/nu, prepared by subcutaneous implantation of human gastric cancer cells, NCI-N87 into the back of nude mice)[2] | | Dosage: | 0, 6.25, 12.5, 25, and 50 mg/kg | | Administration: | Oral gavage, daily for 10-28 days | | Result: | Significantly inhibited the tumor growth in a dose-dependent manner. |
| | IC 50 | EGFR: 1.48 ± 0.0 nM (IC50); HER4: 2.49 ± 0.1 nM (IC50); HER2: 7.15 nM (IC50) |
| | Epertinib hydrochloride Preparation Products And Raw materials |
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