Sapitinib

SKU: orb1301080

Description

Sapitinib (AZD-8931) is a potent, ATP-competitive inhibitor of EGFR, ErbB2, and ErbB3 with single-digit nM IC50 values. It demonstrates superior activity to gefitinib or lapatinib in NSCLC cells and exhibits high selectivity for the ErbB family over kinases like MNK1 and Flt. This compound is a valuable tool for in vitro and in vivo studies exploring ErbB signaling in cancer research.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 848942-61-0
• MW: 473.93
• Purity: 98.89%
• Formula: C₂₃H₂₅ClFN₅O₃
• SMILES: CNC(=O)CN1CCC(CC1)Oc1cc2c(Nc3cccc(Cl)c3F)ncnc2cc1OC
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.22 mM);DMSO:40 mg/mL (84.4 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR:4 nM|ERB3:4 nM|ErbB2:3 nM
• In Vivo:
  Sapitinib reveals antitumor activity in BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts. Sapitinib could reduce p-Akt, Ki67 expression and p-ERK in BT474c xenografts following acute treatment. Sapitinib also causes induction of the M30 apoptosis marker. Furthermore, Sapitinib shows greater proapoptotic effect compared with gefitinib and lapatinib in LoVo xenografts.
• In Vitro:
  Sapitinib shows different potency to NSCLC and SCCHN cell lines. Sapitinib has high sensitivity to PC-9 cells (EGFR activating mutation) with GI50 of 0.1 nM and low activity to NCI-1437 cells with GI50 above 10 μM. Sapitinib exhibits more potency against phospho-EGFR, phospho-erbB2 and phospho-erbB3 than either lapatinib or gefitinib in PE/CA-PJ41, PE/CA-PJ49, DOK and FaDu cells.
• Cell Research:
  To determine the antiproliferative activity against cell lines grown in vitro, AZD8931 is tested in a panel of NSCLC and SCCHN cell lines. Cells are incubated for 96 hours with AZD8931 (0.001-10 μM). Viable cell number is determined by 4 hours of incubation with MTS Colorimetric Assay reagent and absorbance measured at 490 nm on a spectrophotometer. (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

Sapitinib, AZD 8931, AZD8931, AZD-8931, Inhibitor, HER2/ErbB2, HER1, EGFR, Epidermal growth factor receptor, ErbB-1, inhibit

Compound Identifiers

PubChem CID

11488320