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Background Information:
Voruciclib (P1446A-05) is an oral, clinical-stage, potent and selective CDKs (CDKs 9, 6, 4) inhibitor with activity in multiple BRAF-mutant and wild type cell lines. It is currently in clinical trials in combination with BRAF inhibitor (PLX4032) to treat advanced BRAF-mutant melanoma (ref 1). It also potently blocks CDK9 (with sub nanomolar potency), the transcriptional regulator of MCL-1, suppressing MCL-1 expression in cell-based and xenograft models of DLBCL (ref 2).
Reference:
1. Adi Diab, et al, Phase I trial of the CDK 4/6 inhibitor, P1446A-05 (voruciclib) in combination with the BRAF inhibitor (BRAFi), vemurafenib in advanced, BRAF-mutant melanoma, Journal of Clinical Oncology, 2015 ASCO Annual Meeting (May 29 - June 2, 2015), Vol 33, No 15_suppl (May 20 Supplement), 2015: 9076.
2. J. Dey, et al, Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition, Nature, Scientific Reports 7, Article number: 18007 (2017), doi:10.1038/s41598-017-18368-w*A single isomer (out of four). Sophisticated instrumentation, such as NOESY and COSY, has been involved in reaffirmation of the structure.
APIM050069: VORUCICLIB
CAS No.: 1000023-04-0.
Molecular Formula: C22H19ClF3NO5? H2O.
Molecular Weight: 487.9.
Purity: 100% stereomerical purity (Chiral HPLC), 99.5% chem purity (HPLC at 254).
QC: HPLC-MS, 1HNMR, COSY, HSQC, NOESY, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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