CP-673451 | CAS#343787-29-1 | PDGFRα/β Inhibitor

MedKoo Cat#: 524866 | Name: CP-673451

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, and has anti-angiogenic and anti-tumor activity.

Chemical Structure

CP-673451

CAS#343787-29-1

Theoretical Analysis

MedKoo Cat#: 524866

Name: CP-673451

CAS#: 343787-29-1

Chemical Formula: C24H27N5O2

Exact Mass: 417.2165

Molecular Weight: 417.50

Elemental Analysis: C, 69.04; H, 6.52; N, 16.77; O, 7.66

Price and Availability

Size	Price	Availability
10mg	USD 285.00	2 Weeks
25mg	USD 550.00	2 Weeks
50mg	USD 900.00	2 Weeks

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Related CAS #

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Synonym

CP-673451; CP673451; CP 673451; CP-673,451; CP673,451; CP 673,451

IUPAC/Chemical Name

1-(2-(5-(2-Methoxyethoxy)benzimidazol-1-yl)quinolin-8-yl)piperidin-4-ylamine

InChi Key

DEEOXSOLTLIWMG-UHFFFAOYSA-N

InChi Code

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

SMILES Code

NC1CCN(C2=C3N=C(N4C5=CC=C(OCCOC)C=C5N=C4)C=CC3=CC=C2)CC1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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

In vitro activity:

This study investigated the anticancer activity of CP-673451, a potent and selective inhibitor of PDGFRβ, on NSCLC cell lines (A549 and H358) and the potential mechanism. The results showed that inhibition of PDGFRβ by CP-673451 induced a significant increase in cell apoptosis, accompanied by ROS accumulation. Reference: Toxicol Lett. 2018 Oct 1;295:88-98. https://pubmed.ncbi.nlm.nih.gov/29857117/

In vivo activity:

The results showed that low-dose CP-673451 (20 mg/kg) led to a medium suppression of tumor growth, while high-dose CP-673451 (40 mg/kg) strongly inhibited tumor growth in vivo (Figure 5A). Doses of 20 and 40 mg/kg CP-673451 exerted an inhibition of 42.56% and 78.15% at day 10, respectively. Reference: Onco Targets Ther. 2014; 7: 1215–1221. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4090130/

	Solvent	mg/mL	mM
Solubility
	DMF	5.0	11.98
	Ethanol	10.0	23.95
	Ethanol:PBS (pH 7.2) (1:1)	0.5	1.20

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 417.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yang Y, Deng Y, Chen X, Zhang J, Chen Y, Li H, Wu Q, Yang Z, Zhang L, Liu B. Inhibition of PDGFR by CP-673451 induces apoptosis and increases cisplatin cytotoxicity in NSCLC cells via inhibiting the Nrf2-mediated defense mechanism. Toxicol Lett. 2018 Oct 1;295:88-98. doi: 10.1016/j.toxlet.2018.05.033. Epub 2018 May 29. PMID: 29857117. 2. Xi Y, Chen M, Liu X, Lu Z, Ding Y, Li D. 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. doi: 10.2147/OTT.S62946. PMID: 25050066; PMCID: PMC4090130.

In vitro protocol:

In vivo protocol:

1. Xi Y, Chen M, Liu X, Lu Z, Ding Y, Li D. 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. doi: 10.2147/OTT.S62946. PMID: 25050066; PMCID: PMC4090130.

1: Johnson JR, Folestad E, Rowley JE, Noll EM, Walker SA, Lloyd CM, Rankin SM, Pietras K, Eriksson U, Fuxe J. Pericytes contribute to airway remodeling in a mouse model of chronic allergic asthma. Am J Physiol Lung Cell Mol Physiol. 2015 Apr 1;308(7):L658-71. doi: 10.1152/ajplung.00286.2014. Epub 2015 Jan 30. PubMed PMID: 25637607; PubMed Central PMCID: PMC4385988. 2: Ehnman M, Missiaglia E, Folestad E, Selfe J, Strell C, Thway K, Brodin B, Pietras K, Shipley J, Östman A, Eriksson U. Distinct effects of ligand-induced PDGFRα and PDGFRβ signaling in the human rhabdomyosarcoma tumor cell and stroma cell compartments. Cancer Res. 2013 Apr 1;73(7):2139-49. doi: 10.1158/0008-5472.CAN-12-1646. Epub 2013 Jan 21. PubMed PMID: 23338608; PubMed Central PMCID: PMC3672973. 3: Thomson S, Petti F, Sujka-Kwok I, Epstein D, Haley JD. Kinase switching in mesenchymal-like non-small cell lung cancer lines contributes to EGFR inhibitor resistance through pathway redundancy. Clin Exp Metastasis. 2008;25(8):843-54. doi: 10.1007/s10585-008-9200-4. Epub 2008 Aug 12. PubMed PMID: 18696232. 4: Roberts WG, Whalen PM, Soderstrom E, Moraski G, Lyssikatos JP, Wang HF, Cooper B, Baker DA, Savage D, Dalvie D, Atherton JA, Ralston S, Szewc R, Kath JC, Lin J, Soderstrom C, Tkalcevic G, Cohen BD, Pollack V, Barth W, Hungerford W, Ung E. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res. 2005 Feb 1;65(3):957-66. PubMed PMID: 15705896.