PHA-767491

• CAT Number: I005058
• CAS Number: 845714-00-3
• Molecular Formula: C12H11N3O
• Molecular Weight: 213.20
• Purity: ≥95%
• Synonyms: 2-pyridin-4-yl-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
• Target: CDK
• Solubility: in DMSO > 10 mM
• Storage: Store at -20°C
• IC50: 10 nM(Cdc7); 34 nM(Cdk9)
• InChI: InChI=1S/C12H11N3O/c16-12-9-7-11(8-1-4-13-5-2-8)15-10(9)3-6-14-12/h1-2,4-5,7,15H,3,6H2,(H,14,16)
• InChIKey: DKXHSOUZPMHNIZ-UHFFFAOYSA-N
• SMILES: C1CNC(=O)C2=C1NC(=C2)C3=CC=NC=C3

PHA-767491（Cat No.:I005058）is a selective inhibitor of the protein kinase PAK4, which plays a significant role in cancer cell growth, survival, and metastasis. By targeting PAK4, this compound disrupts critical signaling pathways involved in oncogenesis, offering potential therapeutic benefits in various cancers, particularly those exhibiting PAK4 overexpression. Preclinical studies have demonstrated that PHA-767491 can inhibit tumor growth and induce apoptosis in cancer cell lines. Ongoing research aims to further elucidate its mechanisms of action and evaluate its efficacy in combination therapies, positioning it as a promising candidate in targeted cancer treatment.

Reference

[1]. Natoni, Alessandro; Murillo, Laura S.; Kliszczak, Anna E. et al. Mechanisms of Action of a Dual Cdc7/Cdk9 Kinase Inhibitor against Quiescent and Proliferating CLL Cells. Molecular Cancer Therapeutics (2011), 10(9), 1624-1634.
[2]. Swords R, Mahalingam D, O/’Dwyer M, et al. Cdc7 kinase – a new target for drug development. Eur J Cancer. 2010 Jan;46(1):33-40. doi: 10.1016/j.ejca.2009.09.020.
[3]. Montagnoli A, Moll J, Colotta F. Targeting cell division cycle 7 kinase: a new approach for cancer therapy. Clin Cancer Res. 2010 Sep 15;16(18):4503-8. doi: 10.1158/1078-0432.CCR-10-0185. Epub 2010 Jul 20.
[4]. Montagnoli A, Valsasina B, Croci V, et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. doi: 10.1038/nchembio.90.