Oritinib

SKU: orb1301179

Description

Oritinib (SH-1028) is a potent and selective EGFR inhibitor, showing low nanomolar IC50 values against wild-type and various mutant forms, including the resistant T790M variant. It is a research tool for investigating targeted therapies in non-small cell lung cancer, with utility in both in vitro biochemical assays and in vivo preclinical models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2035089-28-0
• MW: 539.67
• Purity: 99.62% (May vary between batches)
• Formula: C₃₁H₃₇N₇O₂
• SMILES: COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1c2CCCCn2c2ccccc12
• Target: EGFR
• Solubility: DMSO:120 mg/mL (222.36 mM)

Bioactivity

• Target IC50:
  EGFR (L861Q):4 nM|EGFR (d746-750):1.4 nM|EGFR (d746-750/T790M):0.89 nM|EGFR (WT):18 nM|EGFR L858R/T790M:0.1 nM|EGFR L858R:0.7 nM
• In Vivo:
  In female mice bearing NCI-H1975 and A431 xenograft models， Oritinib (2.5, 5, and 15 mg/kg; oral) significantly inhibits proliferation of tumor cells with no TKI-induced weight loss. In NCI-H1975 tumor-bearing mice, Oritinib (2.5, 5, and 15 mg/kg; oral) shows good bioavailability(Tmax = 1.5-2 h) and extensive distribution from the plasma to the tissues. The AUC0–t values in plasma are 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively.
• In Vitro:
  Oritinib (0.001, 0.01, 0.1, 1, and 10 μM) selectively inhibits EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50s of 3.932, 9.39 and 7.63 nM, respectively. Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells.

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, non-small cell lung cancer, Irreversible, mutant-selective, EGFR, EGFR (L858R), EGFR (L858R/T790M), EGFR (L861Q), EGFR (wt), EGFR TKI, EGFR-T790M, Epidermal growth factor receptor, ErbB-1, Inhibitor, HER1, Oritinib, third-generation, pharmacodynamics, SH1028, SH-1028, SH 1028

Compound Identifiers

PubChem CID

122666966