Description
Cas:211555-08-7
Product Information:
WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
Chemical Formula: C16H15N3O3
Exact Mass: 297.1113
Molecular Weight: 297.314
Elemental Analysis: C, 64.64; H, 5.09; N, 14.13; O, 16.14
Synonym:
WHI-P180
WHI-P-180
WHI-P 180
WHIP180
WHIP-180
WHIP 180
Janex 3
Janex-3
Janex3
Chemical Name:
3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
InChi Key:
BNDYIYYKEIXHNK-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H15N3O3/c1-21-14-7-12-13(8-15(14)22-2)17-9-18-16(12)19-10-4-3-5-11(20)6-10/h3-9,20H,1-2H3,(H,17,18,19)
Smiles Code:
OC1=CC=CC(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)=C1
Technical Data:
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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 i.v., i.p., or p.o. 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 i.p. bolus doses of 25 mg/kg, inhibits IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis.
References:
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An R, Hagiya Y, Tamura A, Li S, Saito H, Tokushima D, Ishikawa T. Cellular phototoxicity evoked through the inhibition of human ABC transporter ABCG2 by cyclin-dependent kinase inhibitors in vitro. Pharm Res. 2009 Feb;26(2):449-58. doi: 10.1007/s11095-008-9738-5. PubMed PMID: 18841444.
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Slon-Usakiewicz JJ, Dai JR, Ng W, Foster JE, Deretey E, Toledo-Sherman L, Redden PR, Pasternak A, Reid N. Global kinase screening. Applications of frontal affinity chromatography coupled to mass spectrometry in drug discovery. Anal Chem. 2005 Mar 1;77(5):1268-74. PubMed PMID: 15732906.
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Cetkovic-Cvrlje M, Roers BA, Schonhoff D, Waurzyniak B, Liu XP, Uckun FM. Treatment of post-bone marrow transplant acute graft-versus-host disease with a rationally designed JAK3 inhibitor. Leuk Lymphoma. 2002 Jul;43(7):1447-53. PubMed PMID: 12389628.
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Ghosh S, Jennissen JD, Liu XP, Uckun FM. 4-[3-Bromo-4-hydroxyphenyl)amino]-6,7-dimethoxyquinazolin-1-ium chloride methanol solvate and 4-[(3-hydroxyphenyl)amino]-6,7-dimethoxy-1-quinazolinium chloride. Acta Crystallogr C. 2001 Jan;57(Pt 1):76-8. PubMed PMID: 11173405.
Products are for research use only. Not for human use.
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