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

Product information

CAS Number: 1000023-05-1

Molecular Weight: 506.30

Formula: C22H20Cl2F3NO5

Chemical Name: 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]-4H-chromen-4-one hydrochloride

Smiles: Cl.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: QCWRANLELLMJSH-OJMBIDBESA-N

InChi: InChI=1S/C22H19ClF3NO5.ClH/c1-27-5-4-12(14(27)9-28)19-15(29)7-16(30)20-17(31)8-18(32-21(19)20)11-3-2-10(6-13(11)23)22(24,25)26;/h2-3,6-8,12,14,28-30H,4-5,9H2,1H3;1H/t12-,14+;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 250 mg/mL (493.78 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Voruciclib hydrochloride (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes. 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.

Products are for research use only. Not for human use.