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CX-6258

Cat. No. M3146
CX-6258 Structure
Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 230 In stock
50mg USD 680 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). CX-6258 is a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 shows robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. CX-6258 shows dose-dependent efficacy in mice bearing MV-4-11 xenografts, with 45% and 75% TGI at 50 and 100 mg/kg/day, respectively.

Protocol
Cell Experiment
Cell lines MV-4-11, SEM, EOL-1, MOLM-13, PL-21, THP-1, K562, MEG01, HL60 and U266 cells
Preparation method Cell Viability assay.
For proliferation assays, cells were plated at 5,000 to 20,000 cells per well in 96 well plates overnight before treatment for 96 hours with serially diluted compound or vehicle DMSO. Cell viability was measured after the addition of 10 μL Alamar Blue (Invitrogen) for 4 hours at 37˚C. The GI50 was determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment.
Concentrations 0~10 μM
Incubation time 96 h
Animal Experiment
Animal models MV-4-11 xenograft models in nude mice
Formulation H2O
Dosages 50 or 100 mg/kg once daily over a period of 21 days
Administration PO
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 461.94
Formula C26H24ClN3O3
CAS Number 1202916-90-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
Haddach M, et al. ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. PMID: 24900437.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CX-6258 supplier, Pim, inhibitors

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