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品質等級
化驗
≥95% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
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
InChI 密鑰
DEEOXSOLTLIWMG-UHFFFAOYSA-N
生化／生理作用
CP-673451 is an ATP-competitive, potent and selective platelet-derived growth factor receptor inhibitor (PDGFR1 (β)/PDGFR2 (α) IC50 = 1/10 nM with 10 μM ATP; IC50 = 252 nM/c-kit, 450 nM/VEGFR-1/2; >450-fold reduced potency toward other angiogenic receptors and non-receptor kinases). CP-673451 potently inhibits PDGF-BB-induced receptor phosphorylation (IC50 = 6.4 nM; PDGFR1 transfectant) and effectively suppress human cancer xenografts-derived tumor in mice in vivo (ED50 ≤33 mg/kg via b.i.d. or q.d. p.o.) by inhibiting PDGFR phosphorylation and angiogenesis in tumor tissues.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
Feng He et al.
Journal of hepatology, 72(6), 1182-1195 (2020-02-28)
Hepatomegaly can be triggered by insulin and insulin-unrelated etiologies. Insulin acts via AKT, but how other challenges cause hepatomegaly is unknown. Since many hepatomegaly-inducing toxicants and stressors activate NRF2, we examined the effect of NRF2 activation on liver size and
Shuguang Pan et al.
American journal of translational research, 12(7), 3577-3595 (2020-08-11)
Cholangiocarcinoma (CCA) is an aggressive tumour with a poor prognosis due to its late clinical presentation and the lack of effective non-surgical therapies. Previous studies have reported that platelets are implicated in tumour invasion and metastasis, while their role and
W Gregory Roberts et al.
Cancer research, 65(3), 957-966 (2005-02-12)
CP-673,451 is a potent inhibitor of platelet-derived growth factor beta-receptor (PDGFR-beta) kinase- and PDGF-BB-stimulated autophosphorylation of PDGFR-beta in cells (IC(50) = 1 nmol/L) being more than 450-fold selective for PDGFR-beta versus other angiogenic receptors (e.g., vascular endothelial growth factor receptor
Lu Yang et al.
Cell death and differentiation, 27(7), 2066-2080 (2020-01-24)
Lack of insight into the identity of the cells that initiate metastasis hampers the development of antimetastatic therapies. Only a tiny fraction of tumor cells termed metastasis-initiating cells (MICs) are able to successfully seed metastases, causing recurrence and therapeutic resistance.
Yuling Xi et al.
OncoTargets and therapy, 7, 1215-1221 (2014-07-23)
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
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