| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H19ClF3NO5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Voruciclib is an orally active, selective CDK inhibitor with Ki values ranging from 0.626 nM to 9.1 nM. It potently blocks CDK9, the transcriptional regulator of MCL-1, and represses MCL-1 expression in multiple models of diffuse large B-cell lymphoma (DLBCL)[1]. It is supplied as a light yellow to yellow solid (C22H19ClF3NO5, MW 469.84) at 99.76% purity.
Physical & Chemical Properties
| CAS Number | 1000023-04-0 |
|---|---|
| Molecular Formula | C22H19ClF3NO5 |
| Molecular Weight | 469.84 g/mol |
| Purity | 99.76% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | 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 |
| Target | CDK9/cyc T2, CDK9/CycT1, CDK6/cycD1, CDK4/Cyc D1, CDK1/cycB, CDK1/cyc A |
| Signaling Pathway | Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 50 mg/mL (106.42 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
CDK9/cyc T2 0.626 nM (Ki) |
CDK9/CycT1 1.68 nM (Ki) |
CDK6/cycD1 2.92 nM (Ki) |
CDK4/Cyc D1 3.96 nM (Ki) |
CDK1/cycB 5.4 nM (Ki) |
CDK1/cyc A 9.1 nM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (106.42 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
Targeted downregulation of MCL-1 in both ABC and GCB subtypes is shown by Voruciclib (0.5-5 μM; 6 hours)[1]. Voruciclib hydrochloride shows Ki values of 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, and 9.1 nM, respectively, for the targets CDK9/cyc T2 and CDK9/cyc T1, as well as CDK6/cyc D1 and CDK4/cyc D1, plus CDK1/cyc B and CDK1/cyc A[1].
Cell Viability Assay[1]
| Cell Line | U2932, RIVA, OCI-LY10 cells (ABC subtype), NU-DHL-1, SU-DHL-4, SU-DHL-6 cells (GCB subtype) |
|---|---|
| Concentration | 0.5 μM, 1 μM, 2 μM, 3 μM, 4 μM, 5 μM |
| Incubation Time | 6 hours |
| Result | Showed targeted downregulation of MCL-1 in both ABC and GCB subtypes. |
In Vivo
Voruciclib hydrochloride (200 mpk; Oral gavage) combined with Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) gives greater tumor growth inhibition than either drug alone in the U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 (five days per week for 3 weeks) DLBCL models[1].
| Animal Model | ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice |
|---|---|
| Dosage | 200 mpk |
| Administration | Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks) |
| Result | Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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