BI-4142

SKU: orb1686396

Description

BI-4142 is a potent, selective, and orally bioavailable small molecule inhibitor of HER2. It effectively suppresses proliferation in HER2-dependent cell lines and blocks downstream signaling pathways, making it a valuable tool for in vitro and in vivo research in oncology and targeted therapy development.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2682003-36-5
• MW: 521.57
• Purity: 99.84% (May vary between batches)
• Formula: C₂₈H₂₇N₉O₂
• SMILES: O=C(C=C)N1CCN(C2=NC=C3N=CN=C(NC4=CC=C(OC=5C=CC6=C(N=CN6C)C5)C(=C4)C)C3=N2)CC1
• Target: HER,EGFR
• Solubility: DMSO:80 mg/mL (153.38 mM)

Bioactivity

• Target IC50:
  Ba/F3 HER2YVMA cells:18 nM|HEK EGFRWT:270 nM|Ba/F3 EGFRWT cells:2400 nM|HEK HER2YVMA:10 nM|HER2:5 nM
• In Vivo:
  BI-4142 administered at doses ranging from 0 to 100 mg/kg, orally twice daily for 40 days, significantly inhibits tumor growth and suppresses oncogenic signaling.
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• In Vitro:
  BI-4142 inhibits HER2-dependent cell lines and downstream signaling, with IC50 values of 10 nM, 18 nM, 270 nM, and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT, and Ba/F3 EGFRWT, respectively.BI-4142 (1 nM-5 μM, 72 h or 96 h) exhibits antiproliferative activity against tumor cells. In the CaCo-2 assay, BI-4142 displays good permeability and no PgP-mediated efflux liability.
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Storage & Handling

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

Alternative Names

HER2

Compound Identifiers

PubChem CID

156821183