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Synonyms: P1446A | P1446A-05
Compound class: Synthetic organic
Comment: Voruciclib (P1446A, or P1446A-05) is an orally active, non-selective CDK inhibitor that was developed for antineoplastic potential. Potent inhibition of CDK9, 4/6 and 1 by voruciclib is considered as a novel pro-apoptotic mechanism applicable to the treatment of malignant melanoma  and to overcome resistance to Bcl-2 inhibition (e.g. by venetoclax) in B cell malignancies [2,4].
Use of voruciclib in combination with BRAF inhibitors for the treatment of malignant melanoma is claimed in patent US20160136132A1 . Preparation of pure (+)-trans enantiomer of the compound shown here, is claimed in patent WO2007148158A1 .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Agarwal V, Periyasamy G, Rathos M, Srivastava A, Srinivasa S. (2016)
A PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF MELANOMA.
Patent number: US20160136132. Assignee: PIRAMAL ENTERPRISES LIMITED. Priority date: 11/07/2011. Publication date: 19/05/2016.
2. Dey J, Deckwerth TL, Kerwin WS, Casalini JR, Merrell AJ, Grenley MO, Burns C, Ditzler SH, Dixon CP, Beirne E et al.. (2017)
Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition.
Sci Rep, 7 (1): 18007. [PMID:29269870]
3. Eliades P, Miller DM, Miao B, Kumar R, Taylor M, Buch S, Srinivasa SP, Flaherty KT, Tsao H. (2016)
A novel multi-CDK inhibitor P1446A-05 restricts melanoma growth and produces synergistic effects in combination with MAPK pathway inhibitors.
Cancer Biol Ther, 17 (7): 778-84. [PMID:26810603]
4. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV. (2015)
Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells.
PLoS ONE, 10 (11): e0143685. [PMID:26606677]
5. Sivakumar M, Mascarenhas M, Sarde A, Jadhav PK, Shukla M, Joshi K, Rathos M. (2007)
Enantiomerically pure flavone derivatives for the treatment of poliferative disorders and processes for their preparation.
Patent number: WO2007148158A1. Assignee: Piramal Life Sciences Limited. Priority date: 21/06/2006. Publication date: 27/12/2007.