WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206072
Description: Voruciclib, also known as P1446A-05, is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity. CDK4 inhibitor P1446A-05 specifically inhibits CDK4-mediated G1-S phase transition, arresting cell cycling and inhibiting cancer cell growth. The serine/threonine kinase CDK4 is found in a complex with D-type G1 cyclins and is the first kinase to become activated upon mitogenic stimulation, releasing cells from a quiescent stage into the G1/S growth cycling stage; CDK-cyclin complexes have been shown to phosphorylate the retinoblastoma (Rb) transcription factor in early G1, displacing histone deacetylase (HDAC) and blocking transcriptional repression.
MedKoo Cat#: 206072
Chemical Formula: C22H19ClF3NO5
Exact Mass: 469.0904
Molecular Weight: 469.8412
Elemental Analysis: C, 56.24; H, 4.08; Cl, 7.55; F, 12.13; N, 2.98; O, 17.03
Synonym: P1446A05, P1446A-05, P1446A 05, Voruciclib
IUPAC/Chemical Name: 2-(2-Chloro-4-(trifluoromethyl)phenyl)-5,7-dihydroxy-8-((2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-1-benzopyran-4-one
InChi Key: MRPGRAKIAJJGMM-OCCSQVGLSA-N
InChi Code: InChI=1S/C22H19ClF3NO5/c1-27-5-4-12(14(27)9-28)19-15(29)7-16(30)20-17(31)8-18(32-21(19)20)11-3-2-10(6-13(11)23)22(24,25)26/h2-3,6-8,12,14,28-30H,4-5,9H2,1H3/t12-,14+/m1/s1
SMILES Code: O=C1C=C(C2=CC=C(C(F)(F)F)C=C2Cl)OC3=C([C@H]4[C@H](CO)N(C)CC4)C(O)=CC(O)=C13
1: Eliades P, Miller DM, Miao B, Kumar R, Taylor M, Buch S, Srinivasa SP, Flaherty KT, Tsao H. A novel multi-CDK inhibitor P1446A-05 restricts melanoma growth and produces synergistic effects in combination with MAPK pathway inhibitors. Cancer Biol Ther. 2016 Jan 25:0. [Epub ahead of print] PubMed PMID: 26810603.
2: Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV. Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. PLoS One. 2015 Nov 25;10(11):e0143685. doi: 10.1371/journal.pone.0143685. eCollection 2015. PubMed PMID: 26606677; PubMed Central PMCID: PMC4659573.