Home >> CP-673451
Related Products
CP-673451 PDGFRα/β inhibitor,potent and selective

Catalog No.B2173
Size Price Stock Qty
10mM (in 1mL DMSO)
$160.00
In stock
5mg
$119.00
In stock
10mg
$225.00
In stock
50mg
$679.00
In stock
200mg
$2,090.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

CP-673451

Biological Activity

Description CP-673451 is a selective inhibitor of PDGFRα/β with IC50 values of 10 nM/1 nM,respectively.
Targets PDGFRβ PDGFRα c-Kit VEGFR1 VEGFR2  
IC50 1 nM 10 nM 252 nM 450 nM 450 nM  

Protocol

Cell experiment [1]:

Cell lines

PAE-β cells and H526 cells

Preparation method

The solubility of this compound in DMSO is > 20.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0 nM ~ 3 mM

Applications

In PAE-β cells, CP-673451 inhibited PDGFR-β in a dose-dependent manner, with the IC50 value of 6.4nM. CP-673451 also inhibited c-kit in H526 cells, with the IC50 value of 1.1 μM. However, CP-673451 was > 180× selective for PDGFR-β compared with c-kit in H526 cells.

Animal experiment [1]:

Animal models

Mouse sponge angiogenesis model

Dosage form

3, 10 or 30 mg/kg; p.o.; q.d., for 5 days

Applications

CP-673451 (3, 10 or 30 mg/kg; p.o.; q.d., for 5 days) inhibited PDGF-BB-induced angiogenesis by 70 ~ 90%. Corresponding Cmax plasma concentrations after the last dose were 5.5 ~ 419 ng/mL. Besides, CP-673451 showed selective inhibition on PDGF-BB-induced angiogenesis over VEGF- or bFGF-induced angiogenesis (no inhibition observed).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Roberts W G, Whalen P M, Soderstrom E, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer research, 2005, 65(3): 957-966.

CP-673451 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

CP-673451 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 343787-29-1 SDF Download SDF
Chemical Name 1-[2-[5-(2-methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine
Canonical SMILES COCCOC1=CC2=C(C=C1)N(C=N2)C3=NC4=C(C=CC=C4N5CCC(CC5)N)C=C3
Formula C24H27N5O2 M.Wt 417.52
Solubility >20.9mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

CP-673451 is a potent inhibitor of PDGFR with IC50 value of 10nM and 1nM for PDGFR-α and PDGFR-β, respectively [1].

CP-673451 is an ATP-competitive inhibitor and is investigated to treat for cancer. It is highly selective against PDGFR-α and PDGFR-β over a variety of other kinases such as VEGFR-1, VEGFR-2, Lck, TIE-2 and EGFR. In PAE-β cells, CP-673451 inhibits PDGFR-β with IC50 value of 6.4nM. CP-673451 also inhibits c-kit with IC50 value of 1.1μM in H526 cells. In rat C6 glioblastoma xenograft models, a single oral dose of 50mg/kg CP-673451 reduces > 50% phosphorylation of PDGFR-β for 4 hours. In addition, CP-673451 is found to inhibit PDGF-BB-induced angiogenesis in a sponge angiogenesis model. Furthermore, CP-673451 inhibits the tumor growth in Colo205, LS174T, H460, and U87MG xenograft models. It also reduces the microvessel density of Colo205 xenografts [1].

References:
[1] Roberts W G, Whalen P M, Soderstrom E, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer research, 2005, 65(3): 957-966.