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Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]-

Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]- Structure
Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]-
  • CAS No.211555-08-7
  • Chemical Name:Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]-
  • CBNumber:CB02667258
  • Molecular Formula:C16H15N3O3
  • Formula Weight:297.31
  • MOL File:211555-08-7.mol
Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]- Property
  • Boiling point 476.5±40.0 °C(Predicted)
  • Density 1.336±0.06 g/cm3(Predicted)
  • storage temp. 2-8°C(protect from light)
  • solubility DMSO : 25 mg/mL (84.09 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
  • form Powder
  • pka 9.58±0.10(Predicted)
  • color White to off-white
  • UNSPSC Code 12352200
  • NACRES NA.77
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements

Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]- Chemical Properties,Usage,Production

  • Uses WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
  • Biological Activity WHI-P180 is an inhibitor of multiple kinases with IC50 values of 4.5 nM and 66 nM for RET (c-RET) and KDR, respectively.
  • in vivo

    WHI-P180 is also an active inhibitor of IgE-mediated mast cell responses. The elimination half-life of WHI-P180 in CD-1 mice (BALB/c mice) following iv, ip, or po administration is less than 10 min. Systemic clearance of WHI-P180 is 6742 mL/h/kg in CD-I mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic ip bolus doses of 25 mg/kg, inhibits IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis.

  • target
    TargetValue
    RET
    (Cell-free assay)    		 4.5 nM
    KDR
    (Cell-free assay)    		 66 nM
  • IC 50 EGFR: 4 μM (IC50); KDR: 66 nM (IC50); RET: 5 nM (IC50)
  • References [1] Newton R, et al. The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. Eur J Med Chem. 2016 Apr 13;112:20-32. DOI:10.1016/j.ejmech.2016.01.039
    [2] Ghosh S, et al. 4-[3-Bromo-4-hydroxyphenyl)amino]-6,7-dimethoxyquinazolin-1-ium chloride methanol solvateand 4-[(3-hydroxyphenyl)amino]-6,7-dimethoxy-1-quinazolinium chloride. Acta Crystallogr C. 2001 Jan;57(Pt 1):76-8. DOI:10.1107/s0108270100013561
    [3] Chen CL, et al. Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice. Pharm Res. 1999 Jan;16(1):117-22. DOI:10.1023/a:1018835232027
Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]- Preparation Products And Raw materials
Raw materials
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Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]- Spectrum
211555-08-7, Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]-Related Search:
  • Inhibitors
  • 抑制剂
  • 药靶配体
  • 小分子抑制剂，天然产物
  • 小分子抑制剂
  • 化合物WHI-P180,10 MM DMSO 溶液
  • 化合物WHI-P180
  • 3-((6,7-二甲氧基喹唑啉-4-基)氨基)苯酚
  • 3-[(6,7-二甲氧基-4-喹唑啉基)氨基]苯酚, >98%
  • 3-[(6,7-二甲氧基-4-喹唑啉基)氨基]苯酚
  • 211555-08-7
  • WHI-P180, 10 mM in DMSO
  • WHI-P-180,HER1,Janex3,WHI P180,RET,EGFR,Vascular endothelial growth factor receptor,Inhibitor,Janex-3,WHIP180,inhibit,WHI-P180,VEGFR,ErbB-1,Epidermal growth factor receptor
  • WHI-P180, >98%
  • WHI-P180(Janex 3)
  • WHI P180;JANEX3;WHIP180;JANEX-3
  • 3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol (Related Reference)
  • 3-(6,7-dimethoxyquinazolin-4-ylamino)phenol
  • Janex 3
  • 3-[(6,7-Dimethoxy-4-quinazolinyl)amino]phenol
  • Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]-

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