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Chemical Structure| 219580-11-7 Chemical Structure| 219580-11-7
Chemical Structure| 219580-11-7

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CAS No.: 219580-11-7

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PD173074 is an effective FGFR1 inhibitor with an IC50 of 25 nM. It also inhibits the activity of VEGFR2 with an IC50 of 100-200 nM, showing over 1000-fold selectivity for FGFR1 over PDGFR and c-Src.

Synonyms: PD173074

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Product Details of PD173074

CAS No. :219580-11-7
Formula : C28H41N7O3
M.W : 523.67
SMILES Code : O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C
Synonyms :
PD173074
MDL No. :MFCD08705327
InChI Key :DXCUKNQANPLTEJ-UHFFFAOYSA-N
Pubchem ID :1401

Safety of PD173074

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PD173074

RTK

Isoform Comparison

Biological Activity

Target

  • VEGFR2

    VEGFR2, IC50:100 nM-200 nM

  • FGFR1

    FGFR1, IC50:~25 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
mouse embryonic stem cells 100 ng/ml prevent differentiation of mouse embryonic stem cells PMC2667910
Human embryonic stem cells (H1 ESC) 0.1 μM 8 days To study the role of PD173074 in the differentiation of human embryonic stem cells into trophoblast cells, the results showed that PD173074, in combination with BMP4 and A83-01, successfully induced trophoblast differentiation. PMC8411376
CJ7 embryonic stem cells 0.1 μM Used for the culture of embryonic stem cells, inhibiting FGFR activity PMC5461507
Pancreatic stellate cells (PS1 cells) 2 μM 48 h Inhibited nuclear localization of FGFR1 and FGF2, significantly reducing cell proliferation PMC3992074
Pancreatic cancer cells (COLO-357 cells) 2 μM 48 h No effect on nuclear localization of FGFR1 was observed PMC3992074
Human Lung Fibroblasts (HLFs) 0.1 μM 48 h PD173074 inhibited the regulatory effect of FGF2 on the expression of ACTA2, COL1A1, CTGF, LOX, SPRY2, and ETV4 genes. PMC6175645
Human Lung Fibroblasts (HLFs) 0.1 μM 48 h PD173074 inhibited the inhibitory effect of FGF2 on TGF β1-induced expression of COL1A1, LOX, and ACTA2 genes. PMC6175645
MCF7 cells 100 nM 24 to 36 h To investigate the effect of PD173074 on FGF2-induced signaling in MCF7 cells. PMC3005245
T-Rex/K-ras cells 1 μM 24 h PD173074 suppressed K-rasG12V-induced PD-L1 mRNA expression PMC7658718
T-Rex/K-ras cells 1 μM 48 h PD173074 decreased the K-ras-induced expression of PD-L1 protein PMC7658718
MGH-U3 cells 500 nM 2 h Inhibition of FGFR3 activity, leading to decreased MYC protein levels PMC5887543
RT112 cells 500 nM 2 h Inhibition of FGFR3 activity, leading to decreased MYC protein levels PMC5887543

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice MMTV-iFGFR1 mouse model Intraperitoneal injection 1 mg/kg Every 3 days To investigate the effect of PD173074 on iFGFR1 signaling and its role in mammary tumorigenesis. PMC3005245
Mice Prx1Cre;Fgfr3Y367C/+ mouse model Intraperitoneal injection 10 mg/kg Once daily, starting on the day of fracture and continuing until day 7 and 14 post-fracture PD173074 treatment increased cartilage and hypertrophic cartilage volumes in the fracture callus of mutant mice, but did not stimulate cartilage-to-bone transition and did not affect callus and bone volumes. PMC7561512
C57BL/6 mice pancreatic cancer model oral 20 mg/kg once daily for 2 days PD173074 significantly reduced the levels of phosphorylated Akt and PD-L1 protein expression in vivo PMC7658718
mice Tsc1 ?/? mice intraperitoneal injection 20 mg/kg daily for four days inhibited Akt and MAPK activities PMC3633657
Nude mice MGH-U3 and RT112 xenograft models Oral 25 mg/kg Daily for 9 days Inhibition of FGFR3 activity, delayed tumor growth, and decreased expression of both MYC and FGFR3 PMC5887543

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.55mL

1.91mL

0.95mL

19.10mL

3.82mL

1.91mL
Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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