Epertinib hydrochloride

Research use only, not for human use.

Epertinib hydrochloride shows potent antitumor activity.?

Epertinib hydrochloride shows potent antitumor activity.?Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively.

Epertinib hydrochloride inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively.Epertinib hydrochloride shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM.Epertinib hydrochloride (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 hydrochloride (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity.Epertinib hydrochloride (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume.Epertinib hydrochloride (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-22611 hydrochloride

Angiogenesis

EGFR

EGFR|HER4|HER2

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2071195-74-7

596.48

C30H28Cl2FN5O3

>98% (HPLC)

DMSO:125 mg/mL (209.56 mM; Need ultrasonic)

CC#C/C(=N\OC[C@H]1COCCN1)/C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years