AG 490

Pale Yellow-Green Crystal

ChEBI: Tyrphostin B42 is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoic acid with the amino group of benzylamine. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an antioxidant, a STAT3 inhibitor, an anti-inflammatory agent, an apoptosis inducer and a geroprotector. It is an enamide, a monocarboxylic acid amide, a nitrile, a member of catechols and a secondary carboxamide.

A potent and specific inhibitor of the Jak-2 tyrosine kinase.In acute lymphoblastic leukemia (ALL) cells which abundantly express JAK-2, AG-490 dose-dependently inhibited DNA synthesis, blocked cell growth and induced apoptosis. AG-490 does not significantly inhibit other kinases such as Lck, Lyn, Btk, Syk and Src.AG-490 is cell permeable and is active in vivo.

Tyrphostin B42 is used in acute lymphoblastic leukemia studies the compound has been reported to inhibit JAK2 from B cell precursors.

Molecular Weight:294.30
XLogP3:2.4
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:4
Exact Mass:294.10044231
Monoisotopic Mass:294.10044231
Topological Polar Surface Area:93.4
Heavy Atom Count:22
Complexity:460
Undefined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes