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

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

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

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

target

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]-(211555-08-7)Related Product Information

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