CP-673451PDGFRα/β inhibitor,potent and selective CAS# 343787-29-1 |
Quality Control & MSDS
3D structure
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| 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. |
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| 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. |
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| 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. | ||
| 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 | ||
CP-673451 Dilution Calculator
CP-673451 Molarity Calculator
| 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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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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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.
