Riviciclib hydrochloride (P276-00)

For research use only.

Catalog No.S8058

6 publications

Riviciclib hydrochloride (P276-00) Chemical Structure

CAS No. 920113-03-7

Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3.

Selleck's Riviciclib hydrochloride (P276-00) has been cited by 6 publications

1 Customer Review

  • Predicted anticancer drugs inhibit the growth of neuroendocrine tumor cells. Multi-tyrosine kinase inhibitors sorafenib, sunitinib, regorafenib and cabozantinib effectively inhibit GOT1 cell growth with IC50 values in the micromolar range. Inhibitors of AKT (MK-2206), HDAC (vorinostat), HSP90 (alvespimycin) and CDK4/9 (P276-00) also inhibited GOT1 cell growth at micromolar concentrations, whereas inhibition of PARP1 (veliparib) had no effect. GOT1 cells were treated with anticancer drugs at various concentrations for 4 days. Cell viability was estimated using AlamarBlue®. Data points are the mean values of three individual experiments carried out in triplicate (n=9). Fitting of curves was done in GraphPad Prism software v6.04 using log (inhibitor) vs response nonlinear fit with variable slope. IC50 was interpolated at Y=50 and bars denote ±s.d.

    Mod Pathol, 2016, 29(6):616-29. . Riviciclib hydrochloride (P276-00) purchased from Selleck.

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3.
CDK9/CyclinT1 [1] CDK4/CyclinD1 [1] CDK1/CyclinB [1]
CDK2/CyclinA [1] CDK6/CyclinD3 [1]
20 nM 63 nM 79 nM 224 nM 396 nM
In vitro

P276-00 shows 40-fold selectivity toward Cdk4-D1, compared with Cdk2-E[1]. It shows potent antiproliferative effects against various human cancer cell lines, including HCT-116, U2OS, H-460, HL-60, HT-29, SiHa, MCF-7, Colo-205, SW-480, PC-3, Caco2, T-24 with an IC50 ranging from 300 to 800 nmol/L, and is found to be highly selective for cancer cells as compared with normal fibroblast cells[1]. P276-00 can down-regulate cyclin D1 and Cdk4 in an ATP- competitive manner and decrease Cdk4-specific pRb Ser780 phosphorylation. P276-00 also induces apoptosis by actving cellular caspase-3 activity and DNA ladder formation[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-8-5-11 NXP6TmdjeUiWUzDhd5NigQ>? NX;sOmt{WC2pbInjc5Bzd3SnaX6gd5Vje3S{YYTld{Bq\GWwdHnmbYVlKGmwIFvCMVguPS1zMTDh[IVvd2OjcnPpco9u[SClZXzsJIxqdmVuIIHIWHMhfGincnHw[ZV1cWNibHnidoFzgSC|Y4Ll[Y4tKFCxdHXuZ5khRSB3LkG3N|Uh|ryPLh?= NHTuVow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUWxOVI5PCd-M{G1NVUzQDR:L3G+
KB-3-1 MnL4dWhVWyCjc4PhfS=> M13ifXAu\2y7Y3;wdo91\WmwIIP1ZpN1emG2ZYOgbYRmdnSrZnnl[EBqdiCNQj2zMVEh[WSnbn;jZZJkcW6xbXGgZ4VtdCCuaX7lMEByUFSVIITo[ZJieGW3dHnjJIxq[nKjcomgd4Nz\WWwLh?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTVzNUK4OEc,OzF3MUWyPFQ9N2F-

... Click to View More Cell Line Experimental Data

In vivo P276-00, administered i.p. at 50 mg/kg daily for 20 treatments can significantly induce growth inhibition of murine colon cancer (CA-51). However, in murine lung carcinoma model (Lewis lung), an increased dose of 60 mg/kg (30 mg/kg twice daily) administered every alternate day i.p. for 7 treatments shows significant inhibition in the growth[2]. And it also inhibit the growth of human colon carcinoma HCT-116 xenograft and human non-small cell lung carcinoma H-460 xenograft[2]. Efficacy Studies show its maximum tolerated dose is 78 mg/kg/d[2].


Kinase Assay:[1]
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Cdk4-D1/Cdk2-E enzyme assay:

The Cdk4-D1/Cdk2-E enzyme assay is run in 96-well format using Millipore Multiscreen filtration plates. All assay steps are done in a single filter plate. The filtration wells are prewetted with 100 μL of kinase buffer [50 mmol/L HEPES (pH, 7.5), 10 mmol/L MgCl2, 1 mmol/L EGTA], and then the solution is removed by vacuum. With filter plate on vacuum manifold, 50 μL GST-Rb bound to GSH-Sepharose beads in kinase buffer (0.5 μg GST-Rb/50 μL) is added to each well, and vacuum is applied to the filter plate. About 25 μL of a reaction mix containing ATP (cold + hot) and 4× phosphatase inhibitor mix (40 μmol/L unlabeled ATP, 10 μCi/mL γ32P-ATP, 40 mmol/L h-glycerophosphate, 4 mmol/L DTT, 0.4 mmol/L NaF, 0.4 mmol/L sodium orthovanadate) diluted in kinase buffer is added to each well. The test compound (4×final concentration in kinase buffer) or kinase buffer alone (control) is then added in an additional 25 μL volume. To each well, 50 μL (100 ng) of human Cdk4-D1/Cdk2-E enzyme in kinase buffer is added to initiate the reaction, which is allowed to continue for 30 min at 30°C. When the reaction is completed, vacuum is applied again, and the plate is washed with the TNEN buffer [20 mmol/L Tris (pH, 8.0), 100 mmol/L NaCl, 1 mmol/L EDTA, 0.5% nonidet-P40] thrice; the filter plate is air-dried and is placed in a Multiscreen adapter plate. Packard Microscint-O cocktail (30 μL) is added, and the plate is covered with a Top-Seal A film. Quantitation of 32P-GST-Rb in 96-well filter plates is carried out by Top Count scintillation counter. All compounds are tested initially at 1 μmol/L concentration. Compounds showing more than or equal to 50% inhibition are further profiled for IC50 determination.
Cell Research:[1]
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  • Cell lines: HCT-116, U2OS, H-460, HL-60, HT-29, SiHa, MCF-7, Colo-205, SW-480, PC-3, Caco2, T-24
  • Concentrations: ~5.0 μM
  • Incubation Time: 48 h
  • Method: The cells are seeded at a density of 3,000-5,000 cells per well, depending on cell type in 180 μL of culture medium in 96-well plate and incubated overnight to allow the cells to adhere. Varying concentrations of compounds are added to the wells and incubated for 48 h at 37°C. 3H-thymidine (0.25 μCi) is added to each well, and incorporation of the radiolabel is allowed to proceed for 5 to 7 h. Following this incubation, cells are harvested onto GF/B unifilter plates using a Packard Filtermate Universal harvester, and the plates are counted in a Packard Top Count 96-well liquid scintillation counter.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: H-460 xenograft
  • Dosages: 50 mg/kg once daily or 30 mg/kg twice daily
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (200.77 mM)
Water 88 mg/mL (200.77 mM)
Ethanol 7 mg/mL (15.97 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 438.3


CAS No. 920113-03-7
Storage powder
in solvent
Synonyms N/A
Smiles CN1CCC(C1CO)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00899054 Completed Drug: P276-00|Radiation: External beam radiotherapy (EBRT) Squamous Cell Carcinoma of Head and Neck Piramal Enterprises Limited August 2009 Phase 1|Phase 2
NCT00898287 Completed Drug: P276-00|Drug: Gemcitabine Pancreatic Cancer Piramal Enterprises Limited May 2009 Phase 1|Phase 2
NCT00547404 Withdrawn Drug: P276-00 Multiple Myeloma Piramal Enterprises Limited December 2008 Phase 1
NCT00882063 Completed Drug: P276-00 Relapsed and/or Refractory Multiple Myeloma Piramal Enterprises Limited January 2008 Phase 1|Phase 2
NCT00407498 Completed Drug: P276-00 Neoplasm Piramal Enterprises Limited May 2005 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID