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CP 673451

Cat. No. M1941
CP 673451 Structure
Synonym:

CP673451

Size Price Availability Quantity
10mg USD 260 In stock
50mg USD 780 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CP 673451 is a pharmacologically selective PDGFR-beta inhibitor and PDGF-BB-stimulated autophosphorylation of PDGFR-beta in cells (IC50 = 1 nmol/L) being more than 450-fold selective for PDGFR-beta versus other angiogenic receptors. Inhibition of PDGFR-beta phosphorylation in tumors correlates with plasma and tumor levels of CP673451. A dose of 33 mg/kg was adequate to provide >50% inhibition of receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at C(max). In a sponge angiogenesis model, CP 673451 inhibited 70% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg (q.d. x 5, p.o., corresponding to 5.5 ng/mL at C(max)). In vivo, CP 673451 inhibits tumor PDGFR-beta phosphorylation, and it also selectively inhibits PDGF-BB-stimulated angiogenesis. CP 673451 causes significant tumor growth inhibition in multiple human xenograft models.

Protocol
Cell Experiment
Cell lines H526 small cell lung cancer cells
Preparation method For both assays, cells were starved overnight and treated the following day with increasing concentrations of CP-673,451 for 30 minutes at 37°C. During the final 5 to 8 minutes of incubation, either stem cell factor (50 ng/mL) or PDGF-BB (500 ng/mL) was added. Unstimulated cells were used as phosphorylation controls. Cells were washed, lysed, and equivalent protein levels were separated by PAGE. Following transfer to nitrocellulose, membranes were blotted to detect phospho-PDGFR (pY857 antibody, Santa Cruz) or phospho-c-kit (pY719 antibody, Cell Signaling) antibody at 1: 200 overnight at 4°C. Densitometry of bands and IC50 calculation were measured using a LumiImager (Roche, Indianapolis, IN).
Concentrations 0~3000 n M
Incubation time 30 min
Animal Experiment
Animal models Mice bearing Colo205 tumors xenograft model
Formulation 5% Gelucire
Dosages 10, 33, and 100 mg/kg twice daily for 10 days
Administration oral gavage
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 417.5
Formula C24H27N5O2
CAS Number 343787-29-1
Purity >99%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451.
Roberts WG, et al. Cancer Res. 2005 Feb 1;65(3):957-66. PMID: 15705896.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CP 673451, CP673451 supplier, VEGFR/PDGFR, inhibitors

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