Name: Riviciclib hydrochloride (P276-00)
Brand: Selleck Chemicals
SKU: S8058
Availability: InStock
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Quality Control

Batch: S805801 DMSO]88 mg/mL]false]Water]88 mg/mL]false]Ethanol]7 mg/mL]false Purity: 99.26%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.26

Related Targets	HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Other CDK Inhibitors	AS2863619 Ro-3306 SEL120 (SEL120-34A) hydrochloride INX-315 Tagtociclib (PF-07104091) PF-07220060 (CDK4/6-IN-6) AZD4573 ON123300 Enitociclib (BAY 1251152) Samuraciclib (ICEC0942) hydrochloride

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
KB-8-5-11	qHTS assay	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency = 5.1735 μM.	31515284
KB-3-1	qHTS assay	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen.	31515284
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (200.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 88 mg/mL

Ethanol : 7 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (68.45mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	438.3	Formula	C₂₁H₂₀ClNO₅.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	920113-03-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1CCC(C1CO)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl

Mechanism of Action

Targets/IC₅₀/Ki	CDK9/CyclinT1 20 nM CDK4/CyclinD1 63 nM CDK1/CyclinB 79 nM CDK2/CyclinA 224 nM CDK6/CyclinD3 396 nM CDK2/CyclinE 2.54 μM GSK-3β 2.771 μM CDK7/CyclinH 2.87 μM
In vitro	P276-00 shows 40-fold selectivity toward Cdk4-D1, compared with Cdk2-E. 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. This compound can down-regulate cyclin D1 and Cdk4 in an ATP- competitive manner and decrease Cdk4-specific pRb Ser780 phosphorylation. It also induces apoptosis by actving cellular caspase-3 activity and DNA ladder formation.
Kinase Assay	Cdk4-D1/Cdk2-E enzyme assay
Kinase 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.
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. And this compound also inhibit the growth of human colon carcinoma HCT-116 xenograft and human non-small cell lung carcinoma H-460 xenograft. Efficacy Studies show its maximum tolerated dose is 78 mg/kg/d.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17363486/ [2] https://pubmed.ncbi.nlm.nih.gov/17363487/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00899054	Completed	Squamous Cell Carcinoma of Head and Neck	Piramal Enterprises Limited	August 2009	Phase 1\|Phase 2
NCT00898287	Completed	Pancreatic Cancer	Piramal Enterprises Limited	May 2009	Phase 1\|Phase 2
NCT00547404	Withdrawn	Multiple Myeloma	Piramal Enterprises Limited	December 2008	Phase 1
NCT00882063	Completed	Relapsed and/or Refractory Multiple Myeloma	Piramal Enterprises Limited	January 2008	Phase 1\|Phase 2
NCT00407498	Completed	Neoplasm	Piramal Enterprises Limited	May 2005	Phase 1

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Riviciclib hydrochloride (P276-00) CDK inhibitor

Chemical Structure

Molecular Weight: 438.3