Mubritinib

SKU: orb1301053

Description

Mubritinib

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 366017-09-6
• MW: 468.47
• Purity: 99.85%
• Formula: C₂₅H₂₃F₃N₄O₂
• SMILES: FC(F)(F)c1ccc(\C=C\c2nc(COc3ccc(CCCCn4ccnn4)cc3)co2)cc1
• Target: PDGFR,JAK,FGFR,EGFR
• Solubility: 10% DMSO+90% Corn Oil:2 mg/mL (4.27 mM);DMSO:35.1 mg/mL (74.92 mM)

Bioactivity

• Target IC50:
  HER2/ErbB2:6.0 nM
• In Vivo:
  Mubritinib significantly inhibits LN-REC4 xenograft with treatment/control tumor volume ratio of 26.5%. Although i effective to inhibi the growth of UMUC-3 and ACHN cells in vitro IC50 of 1.812 and >25 μM, respectively , oral administration of Mubritinib (10 or 20 mg/kg per day) significantly inhibit the growth of UMUC-3 and ACHN xenografts with treatment/control tumor volume ratio of 22.9% and 26%, respectively as compared with Herceptin (20 mg/kg) which is i effective to UMUC-3 tumor growth.
• In Vitro:
  Mubritinib displays > 4000-fold selectivity over Other tyrosine kinases, such as EGFR, FGFR, PDGFR, Jak1, Src and Blk. Mubritinib even at low concentration of 0.1 μM significantly blocks HER2 phosphorylation, leading to the downregulation of PI3K-Akt and MAPK pathway in cell line BT474 with high level of HER2. Mubritinib not only exhibits highly potent ant Proliferative effect in ErbB2-overexpressing cancer cell line BT474 with an IC50 of 5 nM, but also displays marked ant Proliferative effects in cell lines with HER2 expressed weakly with IC50 of 53 nM, 90 nM and 91 nM for LNCaP, LN-REC4 and T24, respectively Mubritinib displays no inhibitory activities against PC-3 cells with HER2 expressed very faintly with IC50 of 4.62 μM, as well as EGFR-overexpressing HT1376 and ACHN cell lines with IC50 of >25 μM.
• Cell Research:
  Cells are seeded into 6-well plates and cultured overnight. Mubritinib is then added at various concentration , an the cells are treated continuously for 72 hours. Afte the incubation period, cells are counted fo the measurement of ant Proliferative activity.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

PDGFR, JAK1, inhibit, Mubritinib, Inhibitor, HER2/ErbB2, HER1, ErbB-1, Epidermal growth factor receptor, EGFR, FGFR, TAK165, TAK-165, TAK 165

Compound Identifiers

PubChem CID

6444692