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
Appearance: Solid powder
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 469.8412 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.