Epertinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Epertinib (S-222611) 是一种新型强效、口服活性、可逆 EGFR 和 HER2 抑制剂，对 EGFR、HER2 和 HER4 的 IC50 分别为 1.48、7.15 和 2.49 nM。

Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively; does not inhibit KDR, IGF1R, SRC, KIT, PDGFRβ; phosphorylation of EGFR and HER2 kinases in NCI-N87 cells with IC50 of 4.5 and 1.6 nM, shows growth inhibition of NCI-N87 cell with IC50 of 8.3 nM; shows potent antitumor activity over lapatinib in a variety of xenograft models, exhibits excellent activity and could be effective against bone and brain metastasis.Breast Cancer Phase 2 Clinical.

Epertinib inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively.Epertinib shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM. Epertinib (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2.Cell Proliferation Assay Cell Line:NCI-N87 (stomach), BT-474 (breast), SK-BR-3 (breast), MDA-MB-453 (breast), MDA-MB-175VII (breast), HT115 (colon), Calu-3 (lung), fR2 (breast), and MRC-5 (lung)Concentration:0-10 μM Incubation Time:72 h Result:Inhibited the growth of NCI-N87, BT-474, SK-BR-3, MDA-MB-453, MDA-MB-175VII, HT115, Calu-3, fR2, and MRC-5, with IC50 values of 8.3 ± 2.6, 9.9 ± 0.8, 14.0 ± 3.6, 48.6 ± 3.1, 21.6 ± 4.3, 53.3 ± 8.6, 241.5 ± 29.2, 5366.7 ± 65.2, and 4964.6 ± 340.3.

Epertinib (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity.Epertinib (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume.Epertinib (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner. Animal Model:Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)Dosage:12.5, 25, 50, 100 ?mg/kg Administration:Orally, once daily for 28 daysResult: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)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)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.

S-222611 | S222611

Angiogenesis

EGFR

EGFR

Cancer

Breast Cancer

908305-13-5

560.026

C30H27ClFN5O3

>98% (HPLC)

——

CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[C@@H]5NCCOC5

(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

(-20℃)

With Ice Pack

≥ 2 years