PHA-793887

• CAT Number: I004681
• CAS Number: 718630-59-2
• Molecular Formula: C19H31N5O2
• Molecular Weight: 361.50
• Purity: ≥95%
• Synonyms: N-[6,6-dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4-dihydropyrrolo[3,4-c]pyrazol-3-yl]-3-methylbutanamide
• Target: Cyclin-Dependent Kinases
• Solubility: DMSO ≥70mg/mL Water <1.2mg/mL Ethanol ≥70mg/mL
• Storage: 3 years -20C powder
• IC50: 8 nM(for CDK2); 5 nM(for CDK5); 10 nM(for CDK7)

PHA-793887（Cat No.:I004681）is a potent inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK1, CDK2, and CDK9. By inhibiting these kinases, it disrupts the cell cycle and transcriptional processes essential for cancer cell proliferation. PHA-793887 induces cell cycle arrest, primarily in the G1 and G2/M phases, and promotes apoptosis in cancer cells. Its broad inhibition of CDKs makes it a promising candidate for treating various types of cancer, including solid tumors and hematological malignancies. It continues to be studied for its potential in targeted cancer therapies.

Reference

[1]. Locatelli G et al Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study. Mol Cancer Ther. 2010 May;9(5):1265-73.
[2]. Massard C, Soria JC, Anthoney DA, Proctor A, Scaburri A, Pacciarini MA, Laffranchi B, Pellizzoni C, Kroemer G, Armand JP, Balheda R, Twelves CJ.A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected hepatotoxicity in patients with solid tumors.Cell Cycle. 2011 Mar 15;10(6):963-70. Epub 2011 Mar 15.
[3]. Alzani R, Pedrini O, Albanese C, Ceruti R, Casolaro A, Patton V, Colotta F, Rambaldi A, Introna M, Pesenti E, Ciomei M, Golay J.Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models.Exp Hematol. 2010 Apr;38(4):259-269.e2. Epub 2010 Feb 16.
[4]. Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M.Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. Epub 2010 Jan 25.
[5]. Zoubir M, Flament C, Gdoura A, Bahleda R, Litvinova E, Soumelis V, Conforti R, Viaud S, Soria JC, Kroemer G, Zitvogel L, Chaput N.An inhibitor of cyclin-dependent kinases suppresses TLR signaling and increases the susceptibility of cancer patients to herpesviridae.Cell Cycle. 2011 Jan 1;10(1):118-26. Epub 2011 Jan 1.