1000023-04-0
1000023-04-0 structure
- Name: Voruciclib
- Chemical Name: 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one
- CAS Number: 1000023-04-0
- Molecular Formula: C22H19ClF3NO5
- Molecular Weight: 469.83800
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2017-09-29 10:25:44
- Modify Date: 2024-01-10 15:02:15
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Voruciclib is a clinical stage orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1].
| Name | 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one |
|---|---|
| Synonyms |
UNII-W66XP666AM
Voruciclib |
| Description | Voruciclib is a clinical stage orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1]. |
|---|---|
| Related Catalog | |
| Target |
CDK9/cyc T2:0.626 nM (IC50) CDK9/CycT1:1.68 nM (IC50) CDK6/cycD1:2.92 nM (IC50) CDK4/Cyc D1:3.96 nM (IC50) CDK1/cycB:5.4 nM (IC50) CDK1/cyc A:9.1 nM (IC50) |
| In Vitro | Voruciclib (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes[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 | Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL[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. |
| References |
| Molecular Formula | C22H19ClF3NO5 |
|---|---|
| Molecular Weight | 469.83800 |
| Exact Mass | 469.09000 |
| PSA | 94.14000 |
| LogP | 4.26130 |