Zorifertinib

SKU: orb1303946

Description

Zorifertinib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1626387-80-1
• MW: 459.9
• Purity: 99.36%
• Formula: C₂₂H₂₃ClFN₅O₃
• SMILES: N(C=1C2=C(C=C(OC)C(OC(=O)N3[C@H](C)CN(C)CC3)=C2)N=CN1)C4=C(F)C(Cl)=CC=C4
• Target: Apoptosis,EGFR
• Solubility: Ethanol:18 mg/mL (39.14 mM);DMSO:50 mg/mL (108.72 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.35 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR (L858R):0. nM|EGFR (exon 19 deletion):0.2 nM|TK (WT):0. nM
• In Vivo:
  AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy.
• In Vitro:
  In H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on bot the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively showing mo activity on cell proliferation of H838 cells.
• Cell Research:
  Cell proliferation assay is determined by MTS methods. Briefly, cells are seeded in 96-well plates (at a density to allow for logarithmic growth durin the 72 hour assay) and incubated overnight at 37℃nd 5% CO2. Cells are then exposed to concentration of compounds ranging from 30 to 0.0003 mM for 72 hours. Fo the MTS endpoint, cell proliferation is measured b the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent in accordance wit the manufacturer's protocol. Absorbance is measured with a Tecan Ultra instrument. Predose measurements are made, and concentration needed to reduc the growth of treated cells to half that of untreated cells (GI50) Values are determined using absorbance readings.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

AZD 3759, AZD3759, AZD-3759, Inhibitor, HER1, EGFR, EGFR (WT), EGFR (exon 19Del), EGFR (L858R), Epidermal growth factor receptor, ErbB-1, inhibit, Zorifertinib

Compound Identifiers

PubChem CID

78209992