Products

Enzymes for Research, Diagnostic and Industrial Use

Products
Online Inquiry

Our Products Cannot Be Used As Medicines Directly For Personal Use.

24 hour
Promise

Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.

PD173074

Cat No.
CEI-0010
Description
As a selective FGFR1TK inhibitor, PD173074 displayed selective inhibitory activity towards FGFR1 at 26 nM.
CAS No.
219580-11-7
Molecular Weight
523.67
Purity
>99%
Storage
2 years at -20 centigrade
Targets
FGFR1
Molecular Formula
C28H41N7O3
Chemical Name
1-tert-butyl-3-(2-(4-(diethylamino)butylamino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea
Solubility
DSMO 105 mg/mL Water
In vitro
As a selective FGFR1TK inhibitor, PD173074 displayed selective inhibitory activity towards FGFR1TK at 26 nM. PD173074 inhibited the formation of microcapillaries on Matrigel-coated plastic. PD173074 demonstrated (>100 fold) selective growth inhibitory action towards human umbilical vein endothelial cells compared with a panel of tumor cell lines. In vivo anti-angiogenesis studies in mice revealed that oral administration of PD173074 (25-100 mg/kg) generated dose dependent inhibition of angiogenesis. (1) Oligodendrocyte (OL) lineage cells PD173074 can inhibit growth of OL-lineage cells by inhibiting FGF receptor signaling, as migration, proliferation, and differentiation of oligodendrocyte (OL) lineage cells are influenced by fibroblast growth factor-2 (FGF-2) signaling through its receptors (FGFR) FGFR-1, FGFR-2, and FGFR-3. PD173074 effectively antagonized the effect of FGF-2 on proliferation and differentiation of OL progenitors in culture, while platelet-derived growth factor (PDGF)-induced proliferation was unaffected by PD173074. In the same way, mitogen-activated protein kinase (MAPK) activation, a downstream event after activation of either FGFR or PDGFR, was also blocked by PD173074 in OL progenitors stimulated with FGF-2 but not PDGF. PD173074 also completely antagonized two phenotypic alterations of differentiated OLs, specifically downregulation of myelin proteins, and their re-entry into the cell cycle. We conclude that PD173704 is an effective and specific inhibitor for multiple FGF-2-mediated responses of both OL progenitors and differentiated OLs. (2) MM lines PD173074 specifically inhibited the growth of the two t(4;14)-positive MM lines, KMS-11 and OPM-2. PD173074 induced a dose-dependent reduction in cell viability and an increase in apoptosis, accompanied by a decrease in extracellular signal-related kinase phosphorylation. (3) SCLC cells As fibroblast growth factor-2 induces proliferation and chemoresistance in SCLC cells, PD173074 blocks H-510 and H-69 SCLC proliferation and clonogenic growth in a dose-dependent fashion and prevents FGF-2-induced chemoresistance. (4) UC cell lines PD173074 suppressed cell proliferation remarkably in two UC cell lines, UM-UC-14 and MGHU3, which expressed mutated FGFR3 protein. The growth inhibitory effect of PD173074 was associated with arrest at G(1)-S transition in a dose-depending manner. After PD173074 treatment, an inverse relationship between Ki-67 and p27/Kip1 expression suggests that up-regulation of p27 recruited UC cells harboring activating FGFR3 mutations in G(1) that was analogous with the other receptor TKIs acting on the epidermal growth factor receptors.
0
Click unfold / close
Inquiry Basket
Delete selected Quote Check Out
Decide to move out of the shopping cart?
Sure No, Back

Please choose product!

< Go Back
You have already added to buy this product