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Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $147 | In Stock | |
5 mg | $289 | In Stock | |
10 mg | $455 | In Stock | |
25 mg | $889 | In Stock | |
1 mL x 10 mM (in DMSO) | $298 | In Stock |
Description | Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and 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 |
Smiles | CN1CC[C@H]([C@@H]1CO)c1c(O)cc(O)c2c1oc(cc2=O)-c1ccc(cc1Cl)C(F)(F)F |
Relative Density. | 1.493 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 42.5 mg/mL (90.46 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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