Free shipping on all orders over $ 500

PHA-793887

Cat. No. M3475
PHA-793887 Structure
Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 200 In stock
50mg USD 620 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • 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 >98%
Solubility DMSO 70 mg/mL
Storage at -20°C
Related CDK Products
THZ2

THZ2 (an analog of THZ1) is a potent and selective CDK7 inhibitor which overcomes the instability of THZ1 in vivo (IC50s: CDK7=13.9 nM; TNBC cells=10 nM).

LY-3177833

LY-3177833 is a potent and selective inhibitor of CDC7 with IC50 of 3.3 nM.

Voruciclib

Voruciclib (P1446A-05) is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with IC50s of 90nM, 25nM, and 22nM for CDK4-CyclinD1, CDK1-Cyclin B, and CDK9-Cyclin T, respectively.

CVT-313

CVT-313 is a potent and selective inhibitor of CDK2 that prevents neointimal proliferation, which has an IC50 of 0.5 microM in vitro.

ON123300

ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PHA-793887 supplier, CDK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.