HKI 357

DESCRIPTION

An irreversible dual inhibitor of EGFR and HER2 (IC50s = 34 and 33 nM, respectively); inhibits proliferation of A431, SK-BR-3, and SW620 cancer cell lines (IC50s = 120, 2.5, and 511 nM, respectively); suppresses EGFR autophosphorylation and phosphorylation of the downstream effectors AKT and ERK in NCI-H1650 and NCI-H1650(G7) cells; inhibits tumor growth in BT474, A431, and SUM190 mouse xenograft models (10 mg/kg)

DETAILS

Inchi: InChI=1S/C31H29ClFN5O3/c1-4-40-29-16-26-24(15-27(29)37-30(39)9-6-12-38(2)3)31(21(17-34)18-35-26)36-23-10-11-28(25(32)14-23)41-19-20-7-5-8-22(33)13-20/h5-11,13-16,18H,4,12,19H2,1-3H3,(H,35,36)(H,37,39)/b9-6+
Purity: ≥98%
Raptas: Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling
Smiles: O=C(/C=C/CN(C)C)N([H])C1=C(OCC)C=C(N=CC(C#N)=C2N([H])C3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1
Inchikey: NERXPXBELDBEPZ-RMKNXTFCSA-N
Cas Number: 848133-17-5
Formulation: A solid
Storage Temp: -20
Shipping Temp: -20
Formula Markup: C31H29ClFN5O3
Formula Weight: 574.1
Shelf Life Days: 1460