CP-673451
Based on 22 publication(s) in Google Scholar
CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.65%
- CAS. Nr.: 343787-29-1
- Formel: C24H27N5O2
- Molecular Weight:417.50
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CP-673451
More- Nature. 2025 Jul;643(8071):551-561. [Abstract]
- Nat Neurosci. 2024 Aug;27(8):1534-1544. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(21):e20114. [Abstract]
- Redox Biol. 2026 Mar:90:104002. [Abstract]
- Clin Cancer Res. 2019 Feb 1;25(3):1070-1086. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2024 Dec 30:101454. [Abstract]
- Cell Rep. 2023 Jul 16;42(7):112794 [Abstract]
- Br J Cancer. 2024 Jul;131(2):347-360. [Abstract]
- Cancer Cell Int. 2025 Jun 3;25(1):200. [Abstract]
- J Invest Dermatol. 2019 Jul;139(7):1574-1582. [Abstract]
- Glia. 2020 Feb;68(2):345-355. [Abstract]
- CNS Neurosci Ther. 2024 Nov;30(11):e70071. [Abstract]
- Eur J Pharmacol. 2026 Apr 15:1021:178824. [Abstract]
- Cancers (Basel). 2023 Apr 26;15(9):2498. [Abstract]
- FASEB J. 2016 Nov;30(11):3733-3744. [Abstract]
- Cell Tissue Res. 2025 Aug 21. [Abstract]
- Thorac Cancer. 2025 Jan;16(1):e15488. [Abstract]
- Am J Transl Res. 2020 Jul 15;12(7):3577-3595. [Abstract]
- World J Exp Med. 2025 Jun 20;15(2):100443. [Abstract]
- Research Square Preprint. 2024 Nov 28.
- bioRxiv. 2024 Feb 2.
- bioRxiv. 2023 Apr 4.
Customer Validation & Images
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Biologische Aktivität
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PDGFRα 10 nM (IC50) |
PDGFRβ 1 nM (IC50) |
CP-673451 efficiently suppresses the PDGFR downstream signaling pathway. It inhibits phosphorylation of Akt, GSK-3β, p70S6, and S6 in A549 cells in a concentration-dependent manner. CP-673451 (0.0625-4 μM) significantly reduces the viability of NSCLC cell lines A549 and H1299 in a time- and concentration-dependent manner, with IC50s of 0.49 and 0.61 μM, respectively. CP-673451 (1, 4 μM) induces apoptosis in non-small-cell lung cancer cells. CP-673451 (25, 100, or 400 nM) is effective at inhibiting migration and invasion of NSCLC cells by suppression of lamellipodia formation[1]. CP-673451 and crenolanib show selective lethality toward cells with CA. U2OS cells treated with 1 to 4 μM CP-673451 or crenolanib show a ruffled cell surface as a sign for alterations of the cortical actin cytoskeleton. CP-673451 attenuates PDGF-BB-induced signaling, and significantly enhances the phosphorylation of PDGFR-β downstream effectors, Akt and MEK[2]. CP-673,451 (0.5 μM) regulates cell proliferation through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. CP-673,451 impairs rhabdosphere-forming capacity in both RD and RUCH2 cultures[3]. CP-673,451 inhibits PDGFR-β in PAE-β cells with an IC50 value of 6.4 nM. Besides, CP-673,451 incubation in H526 and PAE-β cells results in an IC50 value of 1.1 μM against c-kit[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 343787-29-1
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Appearance Solid
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Molecular Weight 417.50
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Formel C24H27N5O2
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Color White to off-white
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SMILES
NC1CCN(C2=C3N=C(C=CC3=CC=C2)N4C=NC5=CC(OCCOC)=CC=C54)CC1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jul;643(8071):551-561. PMID: 40369078 -
Nat Neurosci
NG2 glia protect against prion neurotoxicity by inhibiting microglia-to-neuron prostaglandin E2 signaling. [Abstract]2024 Aug;27(8):1534-1544. PMID: 38802591 -
Adv Sci (Weinh)
Endothelial PDGF Signaling Dysregulation Impairs Testicular Interstitial Homeostasis in Diabetes. [Abstract]2026 Apr;13(21):e20114. PMID: 41643060 -
Redox Biol
Macrophage AMPK activated by oxidative stress drives profibrotic crosstalk with tubular cells to accelerate renal fibrosis after ischemic and reperfusion injury. [Abstract]2026 Mar:90:104002. PMID: 41621245 -
Clin Cancer Res
Targeting an Autocrine Regulatory Loop in Cancer Stem-like Cells Impairs the Progression and Chemotherapy Resistance of Bladder Cancer. [Abstract]2019 Feb 1;25(3):1070-1086. PMID: 30397177
CP-673451 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2019 Feb 1;25(3):1070-1086. [Abstract]
Western blot analysis of co-IP of endogenous PDGFR or p-LATS1/2 with YAP from OV6+ UMUC3 or J82 cells without or with recombinant PDGF-BB (10 ng/ml) or CP-673451 (500 nM) for 4 days.
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Cell Mol Gastroenterol Hepatol
Sorafenib Promotes Treg Cell Differentiation To Compromise Its Efficacy via VEGFR/AKT/Foxo1 Signaling in Hepatocellular Carcinoma. [Abstract]2024 Dec 30:101454. PMID: 39743020 -
Cell Rep
Activation of GPR44 decreases severity of myeloid leukemia via specific targeting of leukemia initiating stem cells. [Abstract]2023 Jul 16;42(7):112794 PMID: 37459233 -
Br J Cancer
PDZK1 confers sensitivity to sunitinib in clear cell renal cell carcinoma by suppressing the PDGFR-β pathway. [Abstract]2024 Jul;131(2):347-360. PMID: 38822145 -
Cancer Cell Int
Pericytes in castration-resistant prostate cancer associated with disease progression and immunotherapy response: insights from single-cell analysis. [Abstract]2025 Jun 3;25(1):200. PMID: 40462105 -
J Invest Dermatol
Itraconazole Induces Regression of Infantile Hemangioma via Downregulation of the Platelet-Derived Growth Factor-D/PI3K/Akt/mTOR Pathway. [Abstract]2019 Jul;139(7):1574-1582. PMID: 30690033 -
Glia
2020 Feb;68(2):345-355. PMID: 31518022
CP-673451 purchased from MedChemExpress. Usage Cited in: Glia. 2020 Feb;68(2):345-355. [Abstract]
Western blots of PDGFRα and NG2 in slices treated with CP673451 and Crenolanib for 9 days.
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CNS Neurosci Ther
PTP1B Modulates Carotid Plaque Vulnerability in Atherosclerosis Through Rab5-PDGFRβ-Mediated Endocytosis Disruption and Apoptosis. [Abstract]2024 Nov;30(11):e70071. PMID: 39517122 -
Eur J Pharmacol
Nstpbp5185, a novel benzimidazole derivative, suppresses PDGF signaling and reduces neointimal hyperplasia following vascular injury. [Abstract]2026 Apr 15:1021:178824. PMID: 41905443 -
Cancers (Basel)
Advanced Cell Culture Models Illuminate the Interplay between Mammary Tumor Cells and Activated Fibroblasts. [Abstract]2023 Apr 26;15(9):2498. PMID: 37173963 -
FASEB J
Profibrotic up-regulation of glucose transporter 1 by TGF-β involves activation of MEK and mammalian target of rapamycin complex 2 pathways. [Abstract]2016 Nov;30(11):3733-3744. PMID: 27480571
CP-673451 purchased from MedChemExpress. Usage Cited in: FASEB J. 2016 Nov;30(11):3733-3744. [Abstract]
Autocrine activation of receptor tyrosine kinases (RTKs) is required for induction of GLUT1 by TGF-b. Quantitative RT-PCR analysis of 10 ng/mL TGF-b1–stimulated GLUT1 expression (12 h post treatment) in AKR-2B cells in the presence of the PDGFR specific inhibitor, CP673451 (2 μM).
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Cell Tissue Res
2025 Aug 21. PMID: 40839115 -
Thorac Cancer
Establishing a new human lung squamous cell carcinoma cell line, OMUL-1, expressing insulin-like growth factor 1 receptor and programmed cell death ligand 1. [Abstract]2025 Jan;16(1):e15488. PMID: 39552203 -
Am J Transl Res
Platelet-derived PDGF promotes the invasion and metastasis of cholangiocarcinoma by upregulating MMP2/MMP9 expression and inducing EMT via the p38/MAPK signalling pathway. [Abstract]2020 Jul 15;12(7):3577-3595. PMID: 32774720 -
World J Exp Med
2025 Jun 20;15(2):100443. PMID: 40546672 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (239.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (6.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (6.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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 [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3952 mL | 11.9760 mL | 23.9521 mL | 59.8802 mL |
| 5 mM | 0.4790 mL | 2.3952 mL | 4.7904 mL | 11.9760 mL | |
| 10 mM | 0.2395 mL | 1.1976 mL | 2.3952 mL | 5.9880 mL | |
| 15 mM | 0.1597 mL | 0.7984 mL | 1.5968 mL | 3.9920 mL | |
| 20 mM | 0.1198 mL | 0.5988 mL | 1.1976 mL | 2.9940 mL | |
| 25 mM | 0.0958 mL | 0.4790 mL | 0.9581 mL | 2.3952 mL | |
| 30 mM | 0.0798 mL | 0.3992 mL | 0.7984 mL | 1.9960 mL | |
| 40 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4970 mL | |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4790 mL | 1.1976 mL | |
| 60 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9980 mL | |
| 80 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7485 mL | |
| 100 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5988 mL |
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