MW 523.7 Da, Purity >99%. Potent, ATP-competitive fibroblast growth factor receptor 1 (FGFR1) and FGFR3 inhibitor (IC50 values are 21.5 and 5 nM respectively). Shows little activity at EGFR, InsR, MEK and cPKC. Effectively inhibits angiogenesis in vivo. Also impairs tumor growth and inhibits self-renewal of stem cells.
219580-11-7
> 99%
Solid
523.7 Da
C28H41N7O3
1401
Synthetic
ACH, ACLS, AIS, ANDR_HUMAN, AR, AR8, ASV, AW259666, Androgen nuclear receptor variant 2, Androgen receptor, Androgen receptor (dihydrotestosterone receptor; testicular feminization; spinal and bulbar muscular atrophy; Kennedy disease), Atherosclerosis, susceptibility to, included, Avian sarcoma virus, BBDS, BEK, BEK fibroblast growth factor receptor, BFGFR, BFR1, Basic fibroblast growth factor receptor 1, Beta-interferon, C SRC, C-SRC kinase, CD 333, CD 334, CD309, CD309 antigen, CD331, CD332, CD332 antigen, CD333 antigen, CD334 antigen, CDNA FLJ14219 fis clone NT2RP3003800 highly similar to Rattus norvegicus tyrosine protein kinase pp60 c src mRNA, CEK, CEK 2, CEK3, CFD1, CSK_HUMAN, CYTOPLASMIC TYROSINE KINASE, Cellular Yes 1 protein, Chy, Craniofacial dysostosis 1, Csk A, Cytosolic NADP-isocitrate dehydrogenase, DHTR, DKFZp686N23123, DNA binding protein, Dihydro testosterone receptor, Dihydrotestosterone receptor (DHTR), EC 2.7.10.1, EC 2.7.10.2, ECT1, ER, ER-alpha, ER-beta, ER[a], ER[b], ESR, ESR B, ESR BETA, ESR1_HUMAN, ESRA, ESTR B, Epididymis luminal protein 216, Epididymis secretory protein Li 26, Era, Erb, Erb2, Estr, Estra, Estradiol Receptor alpha, Estradiol Receptor beta, Estradiol receptor, Estrogen Receptor 1, Estrogen Receptor 2, Estrogen receptor, Estrogen receptor 1 (alpha), Estrogen receptor 2 (ER beta), Estrogen receptor 2 ER beta, Estrogen receptor alpha, Estrogen receptor beta 4, Estrogen resistance, included, FGF receptor, FGFBR, FGFR1/PLAG1 fusion, FGFR1_HUMAN, FGFR2_HUMAN, FGFR3_HUMAN, FGFR4_HUMAN, FLG, FLK-1, FLK1, mouse, homolog of, FLT, FLT-2, FLT41, FRT, Fetal liver kinase 1, Fibroblast growth factor receptor 2, Fibroblast growth factor receptor 3, Fibroblast growth factor receptor 3 (achondroplasia thanatophoric dwarfism), Fibroblast growth factor receptor 4, Fibroblast interferon, Flt-1, Fms related tyrosine kinase 1, Fms related tyrosine kinase 1 (vascular endothelial growth factor/vascular permeability factor receptor), Fms related tyrosine kinase 1 vascular endothelial growth factor/vascular permeability factor receptor, Fms related tyrosine kinase 4, Fms-like gene, Fms-like tyrosine kinase 1, Fms-like tyrosine kinase 2, Fms-like tyrosine kinase 4, GCCR, GCPS, GCRST, GCR_HUMAN, GLI Kruppel family member GLI 3, GLI Kruppel family member GLI3 (Greig cephalopolysyndactyly syndrome), GLI family zinc finger 3, GLI3 C-terminally truncated form, GLI3 form of 190 kDa, GLI3 form of 83 kDa, GLI3 full length protein, GLI3-190, GLI3-83, GLI3FL, GLI3_HUMAN, GR, Glioma associated oncogene family zinc finger 3, Glucocorticoid receptor, Grl1, HBGFR, HDL cholesterol, augmented response of, to hormone replacement, included, HEL-216, HEL-S-26, HH2, HRTFDS, HSFGFR3EX, HUMARA, HYSP1, HsT441, ICDH, IDCD, IDH, IDH1, IDHC_HUMAN, IDP, IDPC, IFB, IFF, IFN-beta, IFNB 1, IFNB_HUMAN, Interferon beta, Interferon beta 1 fibroblast, Interferon beta precursor, Isocitrate dehydrogenase (NADP(+)) 1 cytosolic, Isocitrate dehydrogenase 1 (NADP+) soluble, Isocitrate dehydrogenase [NADP] cytoplasmic, JTK 2, JTK 4, JWS, Jackson Weiss syndrome, K-sam, KAL2, KD, KGFR, KRD1, Kdr, Kennedy disease (KD), Keratinocyte growth factor receptor, Keratinocyte growth factor receptor 2, Kinase insert domain receptor, Kinase insert domain receptor (a type III receptor tyrosine kinase), LMPH1A, Ly73, MFR 3, MGC112926, MGC117393, MGC154049, MGC20292, MGC96956, Myocardial infarction, susceptibility to, included, N-SAM, NADP dependent isocitrate dehydrogenase cytosolic, NADP dependent isocitrate dehydrogenase peroxisomal, NADP(+)-specific ICDH, NR3A1, NR3A2, NR3C4, Neuronal CSRC tyrosine specific protein kinase, Neuronal SRC, Neuronal proto-oncogene tyrosine-protein kinase Src, Nuclear receptor subfamily 3 group A member 1, Nuclear receptor subfamily 3 group A member 2, Nuclear receptor subfamily 3 group C member 1, Nuclear receptor subfamily 3 group C member 4, Nuclear receptor subfamily 3 group C member 4 (NR3C4), OGD, OTTHUMP00000017718, OTTHUMP00000017719, OTTHUMP00000174476, OTTHUMP00000174477, Oncogene GLI3, Oncogene SRC, Oxalosuccinate decarboxylase, PAP A, PAPB, PCL, PICD, PPD IV, Protein tyrosine kinase, Protein-tyrosine kinase CYL, Protein-tyrosine kinase receptor flk-1, Proto oncogene tyrosine protein kinase, Proto oncogene tyrosine protein kinase YES, Proto-oncogene c-Fgr, Proto-oncogene c-Src, Proto-oncogene c-Yes, Proto-oncogene tyrosine-protein kinase Src, Protooncogene SRC, Protooncogene SRC Rous sarcoma, RNESTROR, SAM 3, SBMA, SMAX1, SRC Oncogene, SRC proto oncogene non receptor tyrosine kinase, SRC_HUMAN, Soluble VEGF receptor 1 14, Soluble VEGFR1 variant 2, Soluble VEGFR1 variant 21, Spinal and bulbar muscular atrophy, Spinal and bulbar muscular atrophy (SBMA), TFM, TK14, TK25, TKF, Testicular Feminization (TFM), Transcriptional activator GLI3, Transcriptional repressor GLI3R, Tyrosine kinase JTK 4, Tyrosine kinase growth factor receptor, Tyrosine kinase pp60c src, Tyrosine kinase related to fibroblast growth factor receptor, Tyrosine protein kinase SRC 1, Tyrosine-protein kinase CSK, Tyrosine-protein kinase FRT, Tyrosine-protein kinase Yes, Tyrosine-protein kinase receptor FLT, Tyrosine-protein kinase receptor FLT4, Tyrosylprotein kinase, V src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog (avian), VEGFR, VEGFR-1, VEGFR-2, VEGFR-3, VGFR1_HUMAN, VGFR2_HUMAN, Vascular endothelial growth factor receptor 1, Vascular endothelial growth factor receptor 2, Vascular endothelial growth factor receptor 3, Vascular endothelial growth factor vascular permeability factor receptor, Vascular permeability factor receptor, Vascular permeability factor receptor 1, Viral oncogene yes 1 homolog 1, YES proto oncogene 1, Src family tyrosine kinase, YES1 proto oncogene, Src family tyrosine kinase, YES_HUMAN, Yamaguchi sarcoma oncogene, Yes 1, Z FGFR 3, Zinc finger protein GLI 3, androgen receptor splice variant 4b, bFGF-R-1, bacteria-expressed kinase, c Yes, c-src tyrosine kinase, fc13h 10, fibroblast growth factor receptor 1, fms-related tyrosine kinase 2, glucocorticoid nuclear receptor variant 1, heparin-binding growth factor receptor, hydroxyaryl-protein kinase, nr3c1, nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor), p60-Src, p60c-src, p61-Yes, pp60c-src, protein tyrosine kinase, receptor like 14, soluble FGFR4 variant 4, soluble VEGFR2, v src avian sarcoma (Schmidt Ruppin A2) viral oncogene homolog, v src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog avian, v yes 1 Yamaguchi sarcoma viral oncogene homolog 1, zgc:154049
MW 523.7 Da, Purity >99%. Potent, ATP-competitive fibroblast growth factor receptor 1 (FGFR1) and FGFR3 inhibitor (IC50 values are 21.5 and 5 nM respectively). Shows little activity at EGFR, InsR, MEK and cPKC. Effectively inhibits angiogenesis in vivo. Also impairs tumor growth and inhibits self-renewal of stem cells.
219580-11-7
> 99%
Solid
523.7 Da
C28H41N7O3
1401
Synthetic
Soluble in DMSO to 100 mM. Soluble in ethanol to 100 mM.
1-(tert-Butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea
Potent, ATP-competitive fibroblast growth factor receptor 1 (FGFR1) and FGFR3 inhibitor (IC50 values are 21.5 and 5 nM respectively). Shows little activity at EGFR, InsR, MEK and cPKC. Effectively inhibits angiogenesis in vivo. Also impairs tumor growth and inhibits self-renewal of stem cells.
CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C
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)
DXCUKNQANPLTEJ-UHFFFAOYSA-N
1-tert-butyl-3-[2-[4-(diethylamino)butylamino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea
Ambient - Can Ship with Ice
+4°C
+4°C
The product can be stored for up to 12 months
This supplementary information is collated from multiple sources and compiled automatically.
Interferon beta Src Glucocorticoid Receptor CSK Estrogen Receptor VEGF Receptor 2 VEGF Receptor 1 Gli3 Androgen Receptor FGFR1 FGFR2 FGFR4 FGFR3 Yes1 and IDH1 represent proteins and receptors playing different mechanical roles. For instance FGFR1 known as Fibroblast Growth Factor Receptor 1 involves signaling pathways controlling cell division and differentiation; it possesses a mass of approximately 115 kDa. FGFR3 another receptor with similar functions is known for its variants like FGFR3 inhibitors impacting certain pathways. These proteins usually express across various tissues playing roles in development and maintenance.
These targets and proteins serve roles in signal transduction and cellular response. They are part of complexes that help the body react to external signals. For example VEGF Receptors 1 and 2 contribute to angiogenesis and vascular maintenance. FGFR3 interacts with inhibitors influencing bone development and maintenance. Androgen and Estrogen Receptors modulate gene expression in response to hormonal signals affecting diverse physiological processes.
Many of these proteins like Src and Yes1 integrate into significant signaling pathways. The MAPK and PI3K/AKT pathways involve multiple targets such as FGFR1 and Glucocorticoid Receptor contributing to cell growth and survival regulation. These pathways often interact with other proteins for coordinated cellular responses allowing complex regulation of different cellular functions.
These proteins connect to certain pathologies through their involvement in critical pathways. For instance FGFR3 and its inhibitors relate to skeletal disorders like achondroplasia. Estrogen Receptor's interaction can link to breast cancer development often alongside Androgen Receptors influencing hormone-driven tumorous growths. Understanding their roles helps in developing targeted therapies for these conditions.
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2D chemical structure image of ab141117, PD 173074, FGFR1 and FGFR3 inhibitor
BT549 cells were incubated at 37°C for 1 hour with vehicle control (0 μM) and different concentrations of PD 173074 (ab141117) in DMSO. Decreased expression of RSK1 p90 (phospho T359 + S363) Anti-RSK1 p90 (phospho T359) antibody [E238] ab32413 correlates with an increase in PD 173074 concentration, as described in literature.
Whole cell lysates were prepared with RIPA buffer (containing protease inhibitors and sodium orthovanadate), 10 μg of each were loaded on the gel and the WB was run under reducing conditions. After transfer the membrane was blocked for an hour using 5% BSA before being incubated with Anti-RSK1 p90 (phospho T359) antibody [E238] ab32413 at 1/5000 dilution and Anti-beta Actin antibody ab8227 at 1 μg/ml overnight at 4°C. Antibody binding was detected using an anti-rabbit antibody conjugated to HRP Goat Anti-Rabbit IgG H&L (HRP) ab97051 at 1/10000 dilution and visualised using ECL development solution.
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