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PD173074

Cat. No. M1875
PD173074 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 40  USD40 In stock
10mg USD 60  USD60 In stock
50mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

PD173074 is a potent and selective, ATP-competitive FGFR1 and FGFR3 inhibitor with IC50 values of 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. FGF receptor (FGFR) inhibitors exert their effects by activating cell surface receptor tyrosine kinases. PD173074 blocks H-510 and H-69 SCLC proliferation and clonogenic growth in a dose-dependent fashion and prevents FGF-2-induced chemoresistance. FGFR1 inhibitor PD 173074 potently and selectively antagonized the neurotrophic and neurotropic actions of FGF-2. PD 173074 displayed 1,000-fold differential IC(50) values for inhibition of FGF-2-stimulated neurite outgrowth in PC12 cells and in granule neurons, and FGF-2-induced mitogen-activated protein kinase (p44/42) phosphorylation. More dramatically, in H-69 xenografts, PD173074 induced complete responses lasting >6 months in 50% of mice.

Customer Product Validations & Biological Datas
Source J Cardiovasc Pharmacol (2015). Figure 5.PD173074
Method Western Blot
Cell Lines B-cell
Concentrations
Incubation Time 1 h
Results Compared with the vehicle group, the ratio of phosphorylated ERK1/2 to total ERK1/2 was significantly decreased after PD173074 treatment.
Protocol (for reference only)
Cell Experiment
Cell lines H510 and H69 cell lines
Preparation method Cell proliferation assay H510 and H69 (1.5 × 104 cells/mL) in SITA were treated with or without FGF-2; PD173074 for the duration and at the concentration highlighted in the figure legends. Cell number was determined by cell counting.
Concentrations 0~1µM
Incubation time 4 days
Animal Experiment
Animal models H510 or H69 cells xenografts tumor bearing mice model
Formulation buffer alone
Dosages 50 mg/kg
Administration oral gavage
Chemical Information
Molecular Weight 523.67
Formula C28H41N7O3
CAS Number 219580-11-7
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shingo Io, et al. Capturing human trophoblast development with naive pluripotent stem cells in vitro

[2] Chuchu Qiao, et al. PD173074 blocks G1/S transition via CUL3-mediated ubiquitin protease in HepG2 and Hep3B cells

[3] Nicole J Chew, et al. FGFR3 signaling and function in triple negative breast cancer

[4] Nagaraju Anreddy, et al. PD173074, a selective FGFR inhibitor, reverses MRP7 (ABCC10)-mediated MDR

[5] Atish Patel, et al. PD173074, a selective FGFR inhibitor, reverses ABCB1-mediated drug resistance in cancer cells

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