Olafertinib

SKU: orb1296096

Description

Olafertinib (RX-518) is an oral, irreversible, and mutant-selective EGFR inhibitor designed to target T790M-mediated resistance in non-small cell lung cancer (NSCLC). It demonstrates potent activity in both cellular assays and in vivo xenograft models, supporting its investigation as a therapeutic agent for EGFR-mutant NSCLC.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1660963-42-7
• MW: 530.57
• Purity: 99.71% (May vary between batches)
• Formula: C₂₉H₂₈F₂N₆O₂
• SMILES: OCCN1CCN(CC1)c1ccc(Nc2ncc3cccc(-c4cccc(NC(=O)C=C)c4)c3n2)c(F)c1F
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.54 mM);DMSO:120 mg/mL (226.17 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  EGFR (WT):689 nM (GI50)|EGFR (L858R/T790M):5 nM (GI50)|EGFR (del19):10 nM (GI50)
• In Vivo:
  CK-101 significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft models, with no activity in the WT EGFR tumor xenograft model.
• In Vitro:
  CK-101 specifically targets the mutant forms of EGFR, including T790M, while exhibiting minimal activity toward WT EGFR. It selectively inhibits cell proliferation of cell lines expressing both the activating (HCC827, IC50 <15 nM) and resistance mutations (NCI-H1975, IC50 <5 nM).
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Storage & Handling

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

Alternative Names

CK 101, CK101, CK-101, EGFR, EGFR (T790M), EGFR-IN-3, Epidermal growth factor receptor, ErbB-1, HER1, Inhibitor, Olafertinib, NSCLC, inhibit, RX 518, RX518, RX-518

Compound Identifiers

PubChem CID

117909640