Cat. No.: HY-10321G

PD173074 (GMP)

PD173074 GMP is PD173074 (HY-10321) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. PD173074 is an orally active FGFR inhibitor that targets the transphosphorylation of FGFR1 and FGFR2 and blocks the FGF signaling pathway. By reducing the phosphorylation level of SMAD2 and altering the expression of Nodal/Activin target genes, PD173074 eliminates endothelial differentiation potential, thereby inhibiting the formation of capillary-like structures. PD173074 blocks the proliferation and colony formation of tumor cells and increases intratumoral cell apoptosis. PD173074 successfully reverses FGF-2-induced chemoresistance to enhance the effect of cisplatin (HY-17394) in small cell lung cancer models. PD173074 can be applied to research related to critical limb ischemia and small cell lung cancer.

For research use only. We do not sell to patients.

CAS No.: 219580-11-7
Formula: C₂₈H₄₁N₇O₃
Molecular Weight:523.67

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PD173074 (GMP) Chemical Structure

CAS No.: 219580-11-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

FGFR1

FGFR2

All TGF-beta/Smad Isoforms :

Smad1
Smad3

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H520	IC₅₀	281 nM Compound: PD173074	Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay	[PMID: 28521156]
RT-112	GI₅₀	0.015 μM Compound: PD173074	Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay	[PMID: 27599742]
SUM185PE	IC₅₀	20 nM Compound: 58; PD173074	Anticancer activity against human SUM185PE cells assessed as cell growth inhibition incubated for 6 days by CellTiter96 analysis Anticancer activity against human SUM185PE cells assessed as cell growth inhibition incubated for 6 days by CellTiter96 analysis	[PMID: 33650861]
SW780	IC₅₀	84.3 nM Compound: PD173074	Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay	[PMID: 28521156]

In Vitro

PD173074 GMP (GMP) (100 nmol/L; 3-hour pre-incubation, followed by 10-day incubation with repeated 3-hour pre-incubations every 3 days) blocks FGF-induced endothelial differentiation of human adipose-derived stem cells, including reducing CD31 and eNOS mRNA expression, preventing capillary-like structure formation on Matrigel, and eliminating eNOS protein expression^[1].
PD173074 GMP (GMP) (200 nM; 6 h) upregulates LEFTY1, LEFTY2, and FST and downregulates CRIPTO, NODAL, INHBA, INHBB, and NANOG in on-feeder human iPSCs, with no effect on NOMO1, NOMO2, NOMO3, NCLN, or OCT4^[2].
PD173074 GMP (GMP) (200 nM; 6 h) downregulates LEFTY1, NODAL, and NANOG and upregulates FST in feeder-less human iPSCs, with no effect on CRIPTO, LEFTY2, or OCT4^[2].
PD173074 GMP (GMP) (200 nM; 2-6 h) induces time-dependent downregulation of LEFTY1 (starting at 2 h), NODAL (at 6 h), LEFTY2 (at 6 h), and NANOG (starting at 4 h) in feeder-less human iPSCs, with no effect on CRIPTO or OCT4 over 6 h^[2].
PD173074 GMP (GMP) (200 nM; 24 h) downregulates CRIPTO, LEFTY1, and NANOG in feeder-less human iPSCs^[2].
PD173074 GMP (GMP) (200 nM; 6 h) reduces phosphorylation of SMAD2 and FGFR in feeder-less human iPSCs, with no effect on total SMAD2/3 or CRIPTO protein levels^[2].
PD173074 GMP (GMP) (200 nM; 6 h) does not change the perinuclear localization of CRIPTO in feeder-less human iPSCs^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[2]

Cell Line:

activin A-pretreated feeder-less human induced pluripotent stem cells (iPSCs)
Concentration:

200 nM
Incubation Time:

6 h (following 24 h pretreatment with 10 ng/mL activin A)
Result:

Significantly increased the relative expression levels of LEFTY1 and LEFTY2.
Significantly decreased the relative expression level of NANOG.
Caused no significant change in the relative expression levels of CRIPTO, NODAL, and OCT4.

Real Time qPCR^[2]

Cell Line:

feeder-less human induced pluripotent stem cells (iPSCs)
Concentration:

200 nM
Incubation Time:

2 h; 4 h; 6 h
Result:

Caused significant downregulation of LEFTY1 expression at 2 h, with further downregulation at 4 h and 6 h.
Significantly downregulated NODAL expression at 6 h.
Significantly downregulated NANOG expression starting at 4 h.
Caused no significant change in CRIPTO or OCT4 expression at any time point up to 6 h.
Downregulated LEFTY2 expression at 6 h.

Western Blot Analysis^[2]

Cell Line:

feeder-less human induced pluripotent stem cells (iPSCs)
Concentration:

200 nM
Incubation Time:

6 h
Result:

Significantly decreased the relative signal strength of phosphorylated SMAD2 (pSMAD2) and phosphorylated FGF receptor (pFGFR; ~60 kDa).
Caused no significant change in the relative signal strength of total SMAD2/3 or CRIPTO (25 kDa).
Did not alter the size or abundance of CRIPTO protein.

In Vivo

PD173074 GMP (50 mg/kg; p.o.; once daily; 28 d) inhibits the growth of xenograft tumors in nude mouse models inoculated with H-510 and H-69 human small cell lung cancer cells, and its efficacy is comparable to that of Cisplatin (HY-17394) in the H-510 model^[3].
PD173074 GMP (50 mg/kg; p.o.; once daily; 14 d): In nude mouse models inoculated with H-69 human small cell lung cancer cells, it reduces intratumoral proliferation in the early stage of treatment, and this change can be detected by [¹⁸F] FLT-PET in vivo imaging between 7 and 14 days of treatment^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nude mice, bearing H-510 human small cell lung cancer xenografts^[3]
Dosage:

50 mg/kg
Administration:

p.o.; once daily; 28 d
Result:

Impaired tumor growth to a similar extent as single-agent cisplatin, increased the median survival of tumor-bearing mice compared with control animals, and did not affect tumor vasculature or lymph node metastasis.

Related Protocols :

Chemical Information

CAS No. 219580-11-7
Molecular Weight 523.67
Formula C₂₈H₄₁N₇O₃
SMILES

O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Khan S, et al. Fibroblast growth factor and vascular endothelial growth factor play a critical role in endotheliogenesis from human adipose-derived stem cells. J Vasc Surg. 2017;65(5):1483-1492. [Content Brief]

[2]. Wakitani S. The FGF receptor inhibitor PD173074 modulates Lefty expression in human induced pluripotent stem cells differently depending on the culture conditions[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 2022, 1869(7): 119260.

[3]. Pardo O E, et al. The fibroblast growth factor receptor inhibitor PD173074 blocks small cell lung cancer growth in vitro and in vivo[J]. Cancer research, 2009, 69(22): 8645-8651.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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PD173074 (GMP)

All TGF-beta/Smad Isoforms