Riviciclib hydrochloride

SKU: orb1685539

Description

Riviciclib hydrochloride

Research Area

Cell Biology

Key Properties

• CAS Number: 920113-03-7
• MW: 438.3
• Purity: 99.51%
• Formula: C₂₁H₂₀ClNO₅·HCl
• SMILES: Cl.CN1CC[C@H]([C@@H]1CO)c1c(O)cc(O)c2c1oc(cc2=O)-c1ccccc1Cl
• Target: Apoptosis,CDK
• Solubility: Ethanol:7 mg/mL (15.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.53 mM);DMSO:82 mg/mL (187.09 mM);H2O:81 mg/mL (184.8 mM)

Bioactivity

• Target IC50:
  CDK9-CyclinH:2.900 μM|CDK6-CyclinD1:0.396 μM|CDK2-CyclinE:2.500 μM|CDK2-CyclinA:0.224 μM|CDK4-CyclinD1:63 nM|CDK1-CyclinB:79 nM|CDK9-CyclinT1:20 nM
• In Vivo:
  Riviciclib, 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 it 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.
• In Vitro:
  Riviciclib 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. Riviciclib can down-regulate cyclin D1 and Cdk4 in an ATP- competitive manner and decrease Cdk4-specific pRb Ser780 phosphorylation. Riviciclib also induces apoptosis by actving cellular caspase-3 activity and DNA ladder formation.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, P276-00, CDK1/CyclinB, CDK, CDK2/CyclinA, CDK6/CyclinD3, CDK4/CyclinD1, CDK9/cyclin T1, Cyclin dependent kinase, Apoptosis, Riviciclib, Riviciclib hydrochloride, Riviciclib Hydrochloride

Compound Identifiers

PubChem CID

23643975