| Identification | Back Directory | [Name]
Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]- | [CAS]
211555-08-7 | [Synonyms]
Janex 3
WHI-P180, >98%
WHI-P180(Janex 3)
WHI P180;JANEX3;WHIP180;JANEX-3
3-(6,7-dimethoxyquinazolin-4-ylamino)phenol
3-[(6,7-Dimethoxy-4-quinazolinyl)amino]phenol
Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]-
3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol (Related Reference) | [Molecular Formula]
C16H15N3O3 | [MDL Number]
MFCD02683970 | [MOL File]
211555-08-7.mol | [Molecular Weight]
297.31 |
| Chemical Properties | Back Directory | [Boiling point ]
476.5±40.0 °C(Predicted) | [density ]
1.336±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [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 |
| Hazard Information | Back Directory | [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]
| Target | Value | 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) | [storage]
Store at -20°C | [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 |
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