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Voruciclib

Catalog No. T10096L CAS 1000023-04-0

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM). Voruciclib represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma. Voruciclib effectively blocks CDK9, the transcriptional regulator of MCL-1.

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Voruciclib, CAS 1000023-04-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 147.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 455.00
25 mg	In stock	$ 893.00
50 mg	In stock	$ 1,360.00
1 mL * 10 mM (in DMSO)	In stock	$ 333.00

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Purity: 99.89%

Biological Description

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Description	Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM). Voruciclib represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma. Voruciclib effectively blocks CDK9, the transcriptional regulator of MCL-1.
Targets&IC50	CDK6-CyclinD1:2.92 nM(Ki), CDK9-CyclinT2:0.626 nM(Ki), CDK4-CyclinD1:3.96 nM(Ki), CDK9-CyclinT1:1.68 nM(Ki), CDK1-CyclinB:5.4 nM(Ki), CDK1-CyclinA:9.1 nM(Ki)
In vitro	Voruciclib hydrochloride has Ki values for CDK inhibitor such as CDK9/cyc T2 of 0.626 nM, CDK9/cyc T1 of 1.68 nM, CDK6/cyc D1 of 2.92 nM, CDK4/cyc D1 of 3.96 nM, CDK1/cyc B of 5.4 nM, and CDK1/cyc A of 9.1 nM[1].Voruciclib (0.5-5 μM; 6 hours) displays targeted downregulation of MCL-1 in both ABC and GCB subtypes[1].
In vivo	In ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice, Combination of 200 mpk Voruciclib hydrochloride and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) causes increase tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4, and NU-DHL-1 models of DLBCL [1].

Molecular Weight	469.84
Formula	C22H19ClF3NO5
CAS No.	1000023-04-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 42.5 mg/mL (90.46 mM)

References and Literature

1. Dey J, et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition. Sci Rep. 2017 Dec 21;7(1):18007.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Anti-Breast Cancer Compound Library Drug Repurposing Compound Library Hematonosis Compound Library ReFRAME Related Library

Related Products

Related compounds with same targets

KenPaullone 7-O-Prenylscopoletin Palbociclib ZNL-05-044 CDK4-IN-1 SB1317 hydrochloride (1204918-72-8(free base)) Lappaol F CDK9-IN-10

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Keywords

Voruciclib 1000023-04-0 Cell Cycle/Checkpoint CDK Cyclin dependent kinase B-cell multiple inhibit diffuse clinical models DLBCL MCL-1 large CDK9 Inhibitor stage orally lymphoma inhibitor

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