WHI-P180

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：

1. 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.

2. 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.

3. 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.

4. 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.