Voruciclib free base · Synonyms: P1446A-05

Voruciclib is a novel multi-CDK inhibitor.

For research use only. Not for human or veterinary use.

Target CDK

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Voruciclib structure

CAS No.: 1000023-04-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 574.00	BP-02317-25mg	In stock	Get quote
50 mg	USD 918.00	BP-02317-50mg	In stock	Get quote
100 mg	USD 1,470.00	BP-02317-100mg	In stock	Get quote
250 mg	USD 2,940.00	BP-02317-250mg	In stock	Get quote
500 mg	USD 4,700.00	BP-02317-500mg	In stock	Get quote
1 g	Inquire	BP-02317-1g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

Voruciclib (P1446A-05) is a novel multi-CDK inhibitor with IC50s of 90nM, 25nM, and 22nM for CDK4-CyclinD1, CDK1-Cyclin B, and CDK9-Cyclin T, respectively. Voruciclib 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.

Biological activity

In Vitro Voruciclib (0.5-5 μM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes[1]. Ki values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively. 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.

Identifiers

SMILES: CN1CC[C@H]([C@@H]1CO)C1=C2OC(=CC(=O)C2=C(O)C=C1O)C1=CC=C(C=C1Cl)C(F)(F)F
InChIKey: MRPGRAKIAJJGMM-OCCSQVGLSA-N

Specifications

MW (average): 469.8380
Formula: C₂₂H₁₉ClF₃NO₅
CAS No.: 1000023-04-0
Physical state: Solid
Color: Light yellow to yellow
Shipping: 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: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, not in water

Documents

References

[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.

Same target

Search CDK

Same research area

Search Cancer