Epertinib hydrochloride

SKU: orb1218489

Description

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.

Key Properties

• CAS Number: 2071195-74-7
• MW: 596.48
• Purity: >98% (HPLC)
• Formula: C₃₀H₂₈Cl₂FN₅O₃
• SMILES: 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
• Target: EGFR
• Solubility: DMSO:125 mg/mL (209.56 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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 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). 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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

S-22611 hydrochloride

Quick Database Links

Gene Symbol

EGFR