| Identification | Back Directory | [Name]
Epertinib hydrochloride | [CAS]
2071195-74-7 | [Synonyms]
S-222611 HCL
Epertinib HCL
S-22611 hydrochloride
Epertinib hydrochloride | [Molecular Formula]
C30H28Cl2FN5O3 | [MDL Number]
MFCD32215297 | [MOL File]
2071195-74-7.mol | [Molecular Weight]
596.48 |
| Hazard Information | Back Directory | [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 (24.1?mg/kg and 26.5?mg/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) | [storage]
Store at -20°C |
|
| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 19945035818 |
| Website: |
http://www.topule.com/ |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
|