1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis

COH29 

Cat. No.: HY-19931 Purity: 98.04%
Handling Instructions

COH29 is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity with an IC50 of 8 μM in KB cell.

For research use only. We do not sell to patients.

COH29 Chemical Structure

COH29 Chemical Structure

CAS No. : 1190932-38-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 388 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

COH29 is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity with an IC50 of 8 μM in KB cell.

IC50 & Target

IC50: 8 μM (RNR, KB cell), 31.57±3.35 μM (RNR, OV90 cell)[2]

In Vitro

COH29 overcome hydroxyurea and gemcitabine resistance in cancer cells. It effectively inhibits proliferation of most cell lines in the NCI 60 human cancer panel, most notably ovarian cancer and leukemia, but exerts little effect on normal fibroblasts or endothelial cells. Site-directed mutagenesis, NMR and surface plasmon resonance biosensor studies confirm COH29 binding to the proposed ligand-binding pocket and offer evidence for assembly blockade of the RRM1-RRM2 quaternary structure[1].

In Vivo

COH29 results in a dose-dependent inhibition of MOLT-4 tumor xenograft growth with twice-daily oral dosing at 50 mg/kg and 100 mg/kg, which is pronounced by Day 12 of treatment. Similarly, 7 days of treatment of mice bearing TOV11D xenografts with 200, 300, or 400 mg/kg/day COH29 results in a dose-dependent inhibition of tumor xenograft growth. Tumor growth is significantly inhibited compared with the control group[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (73.73 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3785 mL 11.8923 mL 23.7846 mL
5 mM 0.4757 mL 2.3785 mL 4.7569 mL
10 mM 0.2378 mL 1.1892 mL 2.3785 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cells is seeded into 96-well plates in 100 µL of complete medium at 2000 to 5000 cells per well, depending on the cell line’s growth rate. After overnight incubation, test compound is added to each well at various concentrations in 50 µL of culture medium. After a further incubation for 96 hours at 37°C, fluorescein diacetate (final concentration: 10 mg/mL) and eosin Y [final concentration: 0.1% (w/v)] is added to each well, and the cells is incubated for an additional 20 minutes at 37°C. Cytotoxicity is assessed by Digital Imaging Microscopy System detection Viability is assessed using MTS [(3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium)] as previously described[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female NSG mice (NOD/SCID/IL2Rgamma null) aged 8-10 weeks are supplied. Each mouse is injected with 5×106Molt-4 or TOV-112D cells subcutaneously in the right flank, and tumor volume is monitored (0.5×l×w2). After the tumors reach approximately 70 mm3, COH29 in 30% solutol is administered daily by gavage in a one or two dose schedule. Mice is sacrificed on the 28th day after cancer cell transplantation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

420.44

Formula

C₂₂H₁₆N₂O₅S

CAS No.

1190932-38-7

SMILES

O=C(NC1=NC(C2=CC=C(O)C(O)=C2)=C(C3=CC=CC=C3)S1)C4=CC=C(O)C(O)=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.04%

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Product Name:
COH29
Cat. No.:
HY-19931
Quantity:

COH29

Cat. No.: HY-19931