WHI-P180

WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.

Product information

CAS Number: 211555-08-7

Molecular Weight: 297.31

Formula: C16H15N3O3

Synonym:

Janex-3

Chemical Name: 3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol

Smiles: COC1=CC2=C(NC3=CC(O)=CC=C3)N=CN=C2C=C1OC

InChiKey: BNDYIYYKEIXHNK-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.