Rociletinib

SKU: orb1305584

Description

Rociletinib

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1374640-70-6
• MW: 555.55
• Purity: 98.52%
• Formula: C₂₇H₂₈F₃N₇O₃
• SMILES: COc1cc(ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F)N1CCN(CC1)C(C)=O
• Target: EGFR
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.94 mM);DMSO:27.78 mg/mL (50 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR (L858R/T790M):21.5 nM(Ki)|EGFR (WT):303.3 nM(Ki)
• In Vivo:
  CO-1686 selectively inhibits the growth of NSCLC (non-small cell lung cancer) cells expressing mutant EGFR, with a GI50 range of 7 to 32 nM, and induces apoptosis. NSCLC cell lines resistant to CO-1686 show signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. In cells expressing mutant EGFR, CO-1686 inhibits p-EGFR with an IC50 range of 62 to 187 nM, while also inhibiting EGFR phosphorylation in three types of cells expressing WT (wild type) EGFR, with an IC50 of >2,000 nM.
• In Vitro:
  CO-1686 demonstrates significant dose-dependent tumor growth inhibition across all models of EGFR mutations, including transgenic mice expressing EGFRL858R- and EGFRL858R/T790M.
• Cell Research:
  Cells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.(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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CO-1686, CNX 419, CNX419, CNX-419, CO 1686, CO1686, AVL 301, AVL301, AVL-301, Inhibitor, inhibit, EGFR, EGFR (L858R/T790M), EGFR (wt), Epidermal growth factor receptor, ErbB-1, HER1, Rociletinib

Compound Identifiers

PubChem CID

57335384