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MedKoo Cat#: 406350 | Name: PD173074
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PD173074 is a small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI), as a therapeutic modality using eight UC cell lines. PD173074 suppressed cell proliferation remarkably in two cell lines, namely, UM-UC-14 and MGHU3, which expressed mutated FGFR3 protein. Cell cycle analysis revealed the growth inhibitory effect of PD173074 was associated with arrest at G(1)-S transition in a dose-depending manner. In the mouse xenograft models using subcutaneously transplanted UM-UC-14 and MGHU3, orally administered PD173074 suppressed tumor growth and induced apoptotic changes comparable with the results of our in vitro assay.

Chemical Structure

PD173074
PD173074
CAS#219580-11-7

Theoretical Analysis

MedKoo Cat#: 406350

Name: PD173074

CAS#: 219580-11-7

Chemical Formula: C28H41N7O3

Exact Mass: 523.3271

Molecular Weight: 523.67

Elemental Analysis: C, 64.22; H, 7.89; N, 18.72; O, 9.17

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,350.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 3,950.00 2 Weeks
2g USD 6,550.00 2 Weeks
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Related CAS #
No Data
Synonym
PD173074; PD 173074; PD-173074.
IUPAC/Chemical Name
1-(tert-butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea
InChi Key
DXCUKNQANPLTEJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H41N7O3/c1-8-35(9-2)13-11-10-12-29-26-30-18-20-16-23(19-14-21(37-6)17-22(15-19)38-7)25(31-24(20)32-26)33-27(36)34-28(3,4)5/h14-18H,8-13H2,1-7H3,(H3,29,30,31,32,33,34,36)
SMILES Code
O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs
Storage Condition
0– 4 oC for short term (weeks to 1 month) or -20 C for long terms (months to years).
Solubility
soluble in DMSO, not soluble in water.
Shelf Life
>2 years if stored properly.
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
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Product Data
Product Data
Instruction
View handling instruction
Biological target:
PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM.
In vitro activity:
The present study shows that the FGFR1 inhibitor PD 173074 potently and selectively antagonized the neurotrophic and neurotropic actions of FGF-2. Nanomolar concentrations of PD 173074 prevented FGF-2, but not insulin-like growth factor-1, support of cerebellar granule neuron survival under conditions of serum/K(+) deprivation; another FGF-2 inhibitor, SU 5402, was effective only at a 1,000-fold greater concentration. Reference: J Neurochem. 2000 Oct;75(4):1520-7. https://pubmed.ncbi.nlm.nih.gov/10987832/
In vivo activity:
This report describes a synthetic compound of the pyrido[2,3-d]pyrimidine class, designated PD 173074, that selectively inhibits the tyrosine kinase activities of the FGF and VEGF receptors. This study shows that systemic administration of PD 173074 in mice can effectively block angiogenesis induced by either FGF or VEGF with no apparent toxicity. Reference: EMBO J. 1998 Oct 15;17(20):5896-904. https://pubmed.ncbi.nlm.nih.gov/9774334/
Solvent mg/mL mM
Solubility
DMSO 52.6 100.43
Ethanol 60.8 116.08
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 523.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Bansal R, Magge S, Winkler S. Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells. J Neurosci Res. 2003 Nov 15;74(4):486-93. doi: 10.1002/jnr.10773. PMID: 14598292. 2. Skaper SD, Kee WJ, Facci L, Macdonald G, Doherty P, Walsh FS. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem. 2000 Oct;75(4):1520-7. doi: 10.1046/j.1471-4159.2000.0751520.x. PMID: 10987832. 3. Trudel S, Ely S, Farooqi Y, Affer M, Robbiani DF, Chesi M, Bergsagel PL. Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Blood. 2004 May 1;103(9):3521-8. doi: 10.1182/blood-2003-10-3650. Epub 2004 Jan 8. PMID: 14715624. 4. Mohammadi M, Froum S, Hamby JM, Schroeder MC, Panek RL, Lu GH, Eliseenkova AV, Green D, Schlessinger J, Hubbard SR. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J. 1998 Oct 15;17(20):5896-904. doi: 10.1093/emboj/17.20.5896. PMID: 9774334; PMCID: PMC1170917.
In vitro protocol:
1. Bansal R, Magge S, Winkler S. Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells. J Neurosci Res. 2003 Nov 15;74(4):486-93. doi: 10.1002/jnr.10773. PMID: 14598292. 2. Skaper SD, Kee WJ, Facci L, Macdonald G, Doherty P, Walsh FS. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem. 2000 Oct;75(4):1520-7. doi: 10.1046/j.1471-4159.2000.0751520.x. PMID: 10987832.
In vivo protocol:
1. Trudel S, Ely S, Farooqi Y, Affer M, Robbiani DF, Chesi M, Bergsagel PL. Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Blood. 2004 May 1;103(9):3521-8. doi: 10.1182/blood-2003-10-3650. Epub 2004 Jan 8. PMID: 14715624. 2. Mohammadi M, Froum S, Hamby JM, Schroeder MC, Panek RL, Lu GH, Eliseenkova AV, Green D, Schlessinger J, Hubbard SR. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J. 1998 Oct 15;17(20):5896-904. doi: 10.1093/emboj/17.20.5896. PMID: 9774334; PMCID: PMC1170917.
1: Logsdon DM, Ming H, Ezashi T, West RC, Schoolcraft WB, Roberts RM, Jiang Z, Yuan Y. Transcriptome comparisons of trophoblasts from regenerative cell models with peri-implantation human embryos. Biol Reprod. 2024 Aug 7:ioae120. doi: 10.1093/biolre/ioae120. Epub ahead of print. PMID: 39109839. 2: Diep CH, Spartz A, Truong TH, Dwyer AR, El-Ashry D, Lange CA. Progesterone Receptor Signaling Promotes Cancer Associated Fibroblast Mediated Tumorigenicity in ER+ Breast Cancer. Endocrinology. 2024 Jul 26;165(9):bqae092. doi: 10.1210/endocr/bqae092. PMID: 39041201. 3: Khan T, Whyte JJ, Schulz LC, Roberts RM. Fluorescence-activated nuclear sorting (FANS) of nuclei from in vitro-generated syncytiotrophoblast. Placenta. 2024 Jun 13:S0143-4004(24)00275-3. doi: 10.1016/j.placenta.2024.06.007. Epub ahead of print. PMID: 38944560. 4: Zeng Q, Hu H, Huang Z, Guo A, Lu S, Tong W, Zhang Z, Shen T. Active and machine learning-enhanced discovery of new FGFR3 inhibitor, Rhapontin, through virtual screening of receptor structures and anti-cancer activity assessment. Front Mol Biosci. 2024 Jun 11;11:1413214. doi: 10.3389/fmolb.2024.1413214. PMID: 38919748; PMCID: PMC11196408. 5: Chao YM, Wu HY, Yeh SH, Yang DI, Her LS, Wu YL. Glucosamine Enhancement of Learning and Memory Functions by Promoting Fibroblast Growth Factor 21 Production. Int J Mol Sci. 2024 Apr 10;25(8):4211. doi: 10.3390/ijms25084211. PMID: 38673797; PMCID: PMC11050103. 6: Du M, Qu Y, Qin L, Zheng J, Sun W. The cell death-related genes machine learning model for precise therapy and clinical drug selection in hepatocellular carcinoma. J Cell Mol Med. 2024 Apr;28(7):e18168. doi: 10.1111/jcmm.18168. PMID: 38494848; PMCID: PMC10945081. 7: Yu IS, Choi J, Kim MK, Kim MJ. The Comparison of Commercial Serum-Free Media for Hanwoo Satellite Cell Proliferation and the Role of Fibroblast Growth Factor 2. Food Sci Anim Resour. 2023 Nov;43(6):1017-1030. doi: 10.5851/kosfa.2023.e68. Epub 2023 Nov 1. PMID: 37969322; PMCID: PMC10636218. 8: Matsuba S, Ura H, Saito F, Ogasawara C, Shimodaira S, Niida Y, Onai N. An optimized cocktail of small molecule inhibitors promotes the maturation of dendritic cells in GM-CSF mouse bone marrow culture. Front Immunol. 2023 Oct 13;14:1264609. doi: 10.3389/fimmu.2023.1264609. PMID: 37901221; PMCID: PMC10611476. 9: Xu T, Zhu Q, Huang Q, Gu Q, Zhu Y, Tang M, Tian S, Wang L, Yan F, Ge J, Sha W, Lin X. FGF21 prevents neuronal cell ferroptosis after spinal cord injury by activating the FGFR1/β-Klotho pathway. Brain Res Bull. 2023 Oct 1;202:110753. doi: 10.1016/j.brainresbull.2023.110753. Epub 2023 Sep 1. PMID: 37660729. 10: Anvar Z, Chakchouk I, Sharif M, Mahadevan S, Su L, Anikar S, Naini FA, Utama AB, Van den Veyver IB. Comparison of Four Protocols for In Vitro Differentiation of Human Embryonic Stem Cells into Trophoblast Lineages by BMP4 and Dual Inhibition of Activin/Nodal and FGF2 Signaling. Reprod Sci. 2024 Jan;31(1):173-189. doi: 10.1007/s43032-023-01334-5. Epub 2023 Sep 1. PMID: 37658178; PMCID: PMC10784360. 11: Shum IO, Merkert S, Malysheva S, Jahn K, Lachmann N, Verboom M, Frieling H, Hallensleben M, Martin U. An Improved Protocol for Targeted Differentiation of Primed Human Induced Pluripotent Stem Cells into HLA-G-Expressing Trophoblasts to Enable the Modeling of Placenta-Related Disorders. Cells. 2023 Aug 15;12(16):2070. doi: 10.3390/cells12162070. PMID: 37626882; PMCID: PMC10453333. 12: Ahmed SM, Ragunathan P, Shin J, Peter S, Kleissle S, Neuenschwander M, Schäfer R, Kries JPV, Grüber G, Dröge P. The FGFR inhibitor PD173074 binds to the C-terminus of oncofetal HMGA2 and modulates its DNA-binding and transcriptional activation functions. FEBS Lett. 2023 Aug;597(15):1977-1988. doi: 10.1002/1873-3468.14675. Epub 2023 Jun 8. PMID: 37259564. 13: Grinchii D, Levin-Greenwald M, Lezmy N, Gordon T, Paliokha R, Khoury T, Racicky M, Herburg L, Grothe C, Dremencov E, Barak S. FGF2 activity regulates operant alcohol self-administration and mesolimbic dopamine transmission. Drug Alcohol Depend. 2023 Jul 1;248:109920. doi: 10.1016/j.drugalcdep.2023.109920. Epub 2023 May 13. PMID: 37224676. 14: Shi T, Hu Z, Tian L, Yang Y. Advances in lung adenocarcinoma: A novel perspective on prognoses and immune responses of CENPO as an oncogenic superenhancer. Transl Oncol. 2023 Aug;34:101691. doi: 10.1016/j.tranon.2023.101691. Epub 2023 May 17. PMID: 37207381; PMCID: PMC10209335. 15: Balasubramanian B, Yacqub-Usman K, Venkatraman S, Myint KZ, Juengsamarn J, Sarkhampee P, Lertsawatvicha N, Sripa J, Kuakpaetoon T, Suriyonplengsaeng C, Wongprasert K, Grabowska AM, Bates DO, Janvilisri T, Tohtong R. Targeting FGFRs Using PD173074 as a Novel Therapeutic Strategy in Cholangiocarcinoma. Cancers (Basel). 2023 Apr 28;15(9):2528. doi: 10.3390/cancers15092528. PMID: 37173994; PMCID: PMC10177182. 16: He D, Ma T, Yi N, Zhang S, Ding G. Significance of PBRM1 mutation in disease progress and drug selection in clear cell renal cell carcinoma. Biotechnol Genet Eng Rev. 2023 Apr 20:1-15. doi: 10.1080/02648725.2023.2204692. Epub ahead of print. PMID: 37079762. 17: Rodrat M, Wongdee K, Chankamngoen W, Teerapornpuntakit J, Thongbunchoo J, Tanramluk D, Charoenphandhu N. Modulation of fibroblast growth factor-23 expression and transepithelial calcium absorption in Caco-2 monolayer by calcium-sensing receptor and calcineurin under calcium hyperabsorptive state. Biochem Biophys Res Commun. 2023 Jun 4;659:105-112. doi: 10.1016/j.bbrc.2023.04.013. Epub 2023 Apr 7. PMID: 37060830. 18: Lu Y, Xu S, Tang R, Han C, Zheng C. A potential link between fibroblast growth factor-23 and the progression of AKI to CKD. BMC Nephrol. 2023 Apr 4;24(1):87. doi: 10.1186/s12882-023-03125-1. PMID: 37016338; PMCID: PMC10074805. 19: Li B, Liang Y, Bao H, Li D, Zhang Y, Dun X, Xu Z, Ji A, Zhang Z, Li Y, Zhang R, Chen W, Zheng Y, Cui L. Real-ambient particulate matter exposure-induced FGFR1 methylation contributes to cardiac dysfunction via lipid metabolism disruption. Sci Total Environ. 2023 Apr 20;870:161903. doi: 10.1016/j.scitotenv.2023.161903. Epub 2023 Jan 31. PMID: 36731555. 20: Pettitt GA, Hurst CD, Khan Z, McPherson HR, Dunning MC, Alder O, Platt FM, Black EV, Burns JE, Knowles MA. Development of resistance to FGFR inhibition in urothelial carcinoma via multiple pathways in vitro. J Pathol. 2023 Feb;259(2):220-232. doi: 10.1002/path.6034. Epub 2022 Dec 13. PMID: 36385700; PMCID: PMC10107504.