Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively.Riviciclib shows antitumor activity on cisplatin-resistant cells.

Product information

CAS Number: 920113-02-6

Molecular Weight: 401.84

Formula: C21H20ClNO5

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

Smiles: CN1CC[C@@H]([C@H]1CO)C1=C2OC(=CC(=O)C2=C(O)C=C1O)C1=CC=CC=C1Cl

InChiKey: QLUYMIVVAYRECT-GXTWGEPZSA-N

InChi: InChI=1S/C21H20ClNO5/c1-23-7-6-12(14(23)10-24)19-15(25)8-16(26)20-17(27)9-18(28-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,14,24-26H,6-7,10H2,1H3/t12-,14+/m0/s1

Technical Data

Appearance: Solid Power

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

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:

Riviciclib (1.5-5 μM; 72 hours) shows no detectable cells in G1 and G2 in promyelocytic leukemia cells and arrest of cells in G1 in synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells. Riviciclib (3-24 hours; 1.5 μM) reduces cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780 decrease at 3 h. Riviciclib shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells.

In Vivo:

Riviciclib (administered i.p.; 35 kg/mg daily for 10 days, in human xenograft mode with severe combined immunodeficient mice) shows significant inhibition in the growth of human colon carcinoma HCT-116 xenograft. Riviciclib (administered via i.p.; 50 mg/kg once daily; 30 mg/kg twice daily for 18 treatments, in human xenograft mode with severe combined immunodeficient mice) significantly inhibits growth.

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