Olmutinib

SKU: orb1300347

Description

Olmutinib (HM61713) is an orally bioavailable, mutant-selective EGFR inhibitor with antineoplastic activity. Its selectivity for mutant EGFR, including T790M, may reduce toxicity relative to non-selective inhibitors. It has demonstrated efficacy in both in vitro assays and in vivo models of non-small cell lung cancer (NSCLC).

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1353550-13-6
• MW: 486.59
• Purity: 99.63%
• Formula: C₂₆H₂₆N₆O₂S
• SMILES: CN1CCN(CC1)c1ccc(Nc2nc(Oc3cccc(NC(=O)C=C)c3)c3sccc3n2)cc1
• Target: EGFR,BTK
• Solubility: DMSO:90 mg/mL (184.96 mM);Ethanol:22 mg/mL (45.21 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (10.28 mM)

Bioactivity

• Target IC50:
  EGFR L858R/T790M:10 nM (cell assay)|EGFR (exon 19 deletion):9.2 nM (cell assay)|BTK:13.9 nM
• In Vivo:
  HM61713 has a half-life of over 24 h for EGFR inhibition. In the in vivo studies of xenograft models with grafts of H1975 and HCC827, HM61713 is active against the tumors without showing any side effects.
• In Vitro:
  HM61713 causes potent inhibition in cell lines H1975 (L858R and T790M) and HCC827 (exon 19 deletion). It has a low potency for NSCLC cell line H358 harboring wild-type EGFR (GI50 of 2225 nM).

Storage & Handling

• Storage: 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

T8460, 1802181-20-9, BI1482694, BI-1482694, BI 1482694, BTK, HER1, Inhibitor, HM 61713, HM61713, HM-61713, HM61713, BI 1482694, HM61713, BI1482694, HM61713, BI-1482694, EGFR, EGFR (cell: H1975), EGFR (cell: HCC827), Epidermal growth factor receptor, ErbB-1, Olmutinib, inhibit

Compound Identifiers

PubChem CID

54758501