Cofttek holdings limited

PDGFR&FGFR

CP-673451 (343787-29-1)

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, has antiangiogenic and antitumor activity.

Not Intended for Therapeutic Use. For research use only.

CAS: 343787-29-1 Category

CP-673451 (343787-29-1) Description:

CP 673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors. In glioblastoma tumors, CP-673451 (33 mg/kg) provides >50% inhibition of PDGFR-β receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at Cmax. In a sponge angiogenesis model, CP-673451 inhibits 70% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg (q.d. ×5, p.o., corresponding to 5.5 ng/mL at Cmax).CP-673451 decreases cell proliferation rate through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. In both RD and RUCH2 cultures, CP-673451 impairs rhabdosphere-forming capacity and cell differentiation, causes increased senescence.

CP 673451 (once-daily p.o. ?0 days dosing routinely) inhibits tumor growth (ED50 < 33 mg/kg) in a number of human tumor xenografts grown s.c. in athymic mice, including H460 human lung carcinoma, Colo205 and LS174T human colon carcinomas, and U87MG human glioblastoma multiforme. In RUCH2 xenograft-bearing mice, CP 673451 reduces tumor growth and stromal cell infiltration.

CP-673451 (343787-29-1) Specifications:

Product Name CP-673451
Synonym CP-673451; CP673451; CP 673451; CP-673,451; CP 673451; CP 673,451
Chemical Name 1-(2-(5-(2-Methoxyethoxy)benzimidazol-1-yl)quinolin-8-yl)piperidin-4-ylamine
Purity ≥98% (HPLC)
CAS Number 343787-29-1
Molecular Formula C24H27N5O2
Molecular Weight 417.513 g/mol
Monoisotopic Mass 417.216 g/mol
MDL number MFCD11100329
InChIKey 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 NC1CCN(C2=C3N=C(N4C5=CC=C(OCCOC)C=C5N=C4)C=CC3=CC=C2)CC1
Form Powder
Color N/A
Solubility  DMSO 84 mg/mL (201.20 mM)

Water Insoluble

Alcohol 60 mg/mL (143.71 mM)

Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application selective inhibitor of PDGFRα/β

 


=

RIDADR NONH for all modes of transport

References:

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

[2]. CP-673451, a platelet-derived growth-factor receptor inhibitor, suppresses lung cancer cell proliferation and migration. Xi Y, Chen M, Liu X, Lu Z, Ding Y, Li D. Onco Targets Ther. 2014 Jul 3;7:1215-21. doi: 10.2147/OTT.S62946. eCollection 2014. PMID: 25050066

[3]. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. 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. Cancer Res. 2005 Feb 1;65(3):957-66. PMID: 15705896

[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.

[5]. 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.

1 review for CP-673451 (343787-29-1)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The CP-673451 (343787-29-1) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *