CP-673451

PDGFRα/β inhibitor,potent and selective CAS# 343787-29-1

CP-673451

Catalog No. BCC4981----Order now to get a substantial discount!

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Quality Control of CP-673451

Number of papers citing our products

Chemical structure

CP-673451

3D structure

Chemical Properties of CP-673451

Cas No. 343787-29-1 SDF Download SDF
PubChem ID 10158940 Appearance Powder
Formula C24H27N5O2 M.Wt 417.52
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (239.52 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-[2-[5-(2-methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine
SMILES COCCOC1=CC2=C(C=C1)N(C=N2)C3=NC4=C(C=CC=C4N5CCC(CC5)N)C=C3
Standard InChIKey DEEOXSOLTLIWMG-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H27N5O2/c1-30-13-14-31-19-6-7-21-20(15-19)26-16-29(21)23-8-5-17-3-2-4-22(24(17)27-23)28-11-9-18(25)10-12-28/h2-8,15-16,18H,9-14,25H2,1H3
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CP-673451

DescriptionCP-673451 is a selective inhibitor of PDGFRα/β with IC50 values of 10 nM/1 nM,respectively.
TargetsPDGFRβPDGFRαc-KitVEGFR1VEGFR2  
IC501 nM10 nM252 nM450 nM450 nM  

Protocol

Cell Assay [3]
Cell proliferation/viability is analyzed using the CyQuant proliferation assay. Pre-starved cells are treated every 24 hours with vehicle (dimethyl sulfoxide) or 0.5 μM CP-673,451 diluted in serum-reduced medium (1.5 % FBS) for 96 hours. The amount of nucleic acid present in lysed cells is normalized to the amount when treatment is initiated. Cell proliferation/viability in response to 300 ng/mL PDGF-CC is likewise analyzed, but cells are then kept in serum-free medium and treated twice during a 48-hour period.

Animal Administration [1]
A subcutaneous A549 xenograft model in nude mice is used to evaluate the anticancer activity of CP-673451. Briefly, A549 cells are injected into the axillary regions of mice (2×106 cells/mouse). When the tumor volumes reach 70 mm3, the mice are randomly assigned to a control group and two CP-673451 groups (n=6 per group): low-dose (20 mg/kg) and high dose (40 mg/kg) groups (vehicle 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300). These animals are administered intraperitoneally with CP-673451 (20 or 40 mg/kg/day) or with vehicle. During the treatment period, the implanted tumors are measured by caliper once a day in a blind fashion. The animal body weights are also measured at the same time. The tumor volume is calculated. After treatment, the mice are killed, and the tumors are harvested and analyzed.

References:
[1]. Xi Y, et al. CP-673451, a platelet-derived growth-factor receptor inhibitor, suppresses lung cancer cell proliferation and migration. Onco Targets Ther. 2014 Jul 3;7:1215-21. [2]. Konotop G, et al. Pharmacological Inhibition of Centrosome Clustering by Slingshot-Mediated Cofilin Activation and Actin Cortex Destabilization. Cancer Res. 2016 Nov 15;76(22):6690-6700. [3]. Ehnman M, et al. Distinct effects of ligand-induced PDGFRα and PDGFRβ signaling in the human rhabdomyosarcoma tumor cell and stroma cell compartments. Cancer Res, 2013, 73(7), 2139-2149. [4]. Roberts WG, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res, 2005, 65(3), 957-966.

CP-673451 Dilution Calculator

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CP-673451 Molarity Calculator

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Preparing Stock Solutions of CP-673451

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3951 mL 11.9755 mL 23.9509 mL 47.9019 mL 59.8774 mL
5 mM 0.479 mL 2.3951 mL 4.7902 mL 9.5804 mL 11.9755 mL
10 mM 0.2395 mL 1.1975 mL 2.3951 mL 4.7902 mL 5.9877 mL
50 mM 0.0479 mL 0.2395 mL 0.479 mL 0.958 mL 1.1975 mL
100 mM 0.024 mL 0.1198 mL 0.2395 mL 0.479 mL 0.5988 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CP-673451

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.

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References on CP-673451

CP-673451, a platelet-derived growth-factor receptor inhibitor, suppresses lung cancer cell proliferation and migration.[Pubmed:25050066]

Onco Targets Ther. 2014 Jul 3;7:1215-21.

Lung cancer is the leading cause of cancer mortality in the world. Although some advances in lung cancer therapy have been made, patient survival is still poor. The platelet-derived growth factor receptors (PDGFRs) and their ligands play critical roles in the regulation of many cancer cell processes, including cell survival and cell motility. Herein, we investigate the anticancer activities of CP-673451, a potent selective inhibitor of PDGFR kinase, in non-small-cell lung cancer (NSCLC) therapy. We found that CP-673451 is effective at suppressing cell viability, inducing cell apoptosis, and inhibiting cell migration and invasion by suppressing the PDGFR downstream signaling pathway in NSCLC cells. Furthermore, CP-673451 is effective at suppressing NSCLC tumor growth in vivo. In summary, our studies suggest that CP-673451 might be a promising therapeutic compound for NSCLC.

Description

CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.

Keywords:

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