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PCI-24781

Cat. No. M1813
PCI-24781 Structure
Synonym:

CRA-024781

Size Price Availability Quantity
10mg USD 140 In stock
50mg USD 400 In stock
100mg USD 600 In stock
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Quality Control
Biological Activity

PCI-24781 is a broad-spectrum phenyl hydroxamic acid HDAC inhibitor with chemotherapy for the treatment of soft tissue sarcoma. PCI-24781 exhibited significant anti-STS proliferative activity in vitro, inducing S phase depletion, G(2)/M cell cycle arrest, and increasing apoptosis. Superior effects were seen when combined with chemotherapy. A PCI-24781-induced reduction in Rad51, a major mediator of DNA double-strand break homologous recombination repair, was shown and may be a mechanism underlying PCI-24781 chemosensitization. We showed that PCI-24781 transcriptionally represses Rad51 through an E2F binding-site on the Rad51 proximal promoter. Although single-agent PCI-24781 had modest effects on STS growth and metastasis, marked inhibition was observed when combined with chemotherapy.

Protocol
Cell Experiment
Cell lines HCT-116, DLD-1, HCT-15, MCF-7, BT-549, NCI-H226, CWR-22RV1, NCI-PC3, SKOV-3, OVCAR-3 and HUVEC cells line
Preparation method Cell Proliferation Assay
Ten tumor cell lines and HUVEC were cultured for at least two doubling times, and growth was monitored at the end of compound exposure using an Alamar blue (Biosource, Camarillo, CA) fluorometric cell proliferation assay as previously described (13). The compound was assayed in triplicate wells in 96-well plates at nine concentrations using half-log intervals ranging from 0.0015 to 10 μmol/L. The final DMSO concentration in each well was 0.15%. The concentration required to inhibit cell growth by 50% (GI50%) and 95% confidence intervals were estimated from nonlinear regression using a four-parameter logistic equation.
Concentrations 0.15 to 3.09 μ M
Incubation time 72 h
Animal Experiment
Animal models HCT116 and DLD-1 tumor -bearing Female BALB/c nu/nu mice
Formulation 20% HP-β-cyclodextrin in water
Dosages q.d. × 4 per week
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 397.42
Formula C21H23N3O5
CAS Number 783355-60-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo.
Buggy JJ, et al. Mol Cancer Ther. 2006 May;5(5):1309-17. PMID: 16731764.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PCI-24781, CRA-024781 supplier, HDAC, inhibitors

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