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PHA-793887

Cat. No. M3475
PHA-793887 Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 250 In stock
50mg USD 750 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PHA-793887 is a novel pan-cdk inhibitor, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range. It is inactive against other 34 kinases representative of all kinase families, in particular c-abl, c-kit, lck, and TRKA with IC50>10 mM. It shows anti-proliferative activity against several solid tumor cell lines, with IC50<1 mM. In these cells, it is able to inhibit Rb phosphorylation and expression of S-phase cyclins, such as cyclin A. [1,2]

Protocol
Cell Experiment
Cell lines A2780 cells
Preparation method Seeding cells into 96- or 384-wells plates at final concentration ranging from 1 ×104 to 3 ×104 per cm2. 24 hours later,using serial dilution of PHA-793887 to treat cells . At 72 hours after the treatment, using the CellTiter-Glo assay to evaluate the amount of cells . using a sygmoidal fit to calculate IC50 values
Concentrations 0.1 nM-1 μM, dissolved in DMSO
Incubation time 72 hours
Animal Experiment
Animal models Mouse xenograft models of human ovarian A2780, colon HCT-116 and pancreatic BX-PC3 carcinoma
Formulation Dissolved in 5% dextrose solution
Dosages 10, 20, and 30 mg/kg
Administration Intravenous injection once daily
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 361.48
Formula C19H31N5O2
CAS Number 718630-59-2
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PHA-793887 supplier, CDK, inhibitors

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