Recombinant Human Fibroblast growth factor receptor 1 (FGFR1), partial

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Code CSB-EP008642HUa0
Size $224
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  • (Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel.

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Product Details

Purity
Greater than 85% as determined by SDS-PAGE.
Target Names
FGFR1
Uniprot No.
Research Area
Cancer
Alternative Names
Basic fibroblast growth factor receptor 1; bFGF-R-1; BFGFR; CD331; CEK; FGFBR; FGFR 1; FGFR-1; FGFR1; FGFR1/PLAG1 fusion; FGFR1_HUMAN; fibroblast growth factor receptor 1; FLG; FLT-2; FLT2; Fms-like gene; Fms-like tyrosine kinase 2; fms-related tyrosine kinase 2; HBGFR; heparin-binding growth factor receptor; HH2; HRTFDS; hydroxyaryl-protein kinase; KAL2; N-SAM; OGD; Proto-oncogene c-Fgr
Species
Homo sapiens (Human)
Source
E.coli
Expression Region
22-376aa
Target Protein Sequence
RPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDDVQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSDALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPSSGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSINHTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKIGPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLEALEERPAVMTSPLYLE
Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
Mol. Weight
43.4 kDa
Protein Length
Extracellular Domain
Tag Info
N-terminal 6xHis-tagged
Form
Liquid or Lyophilized powder
Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.
Buffer
If the delivery form is liquid, the default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol.
Note: If you have any special requirement for the glycerol content, please remark when you place the order.
If the delivery form is lyophilized powder, the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
Reconstitution
We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. Our default final concentration of glycerol is 50%. Customers could use it as reference.
Troubleshooting and FAQs
Storage Condition
Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
Shelf Life
The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
Lead Time
3-7 business days
Notes
Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
Datasheet & COA
Please contact us to get it.
Description

The gene responsible for the Human FGFR1 protein (22-376aa) is incorporated into a plasmid vector, forming recombinant plasmid. The resulting recombinant plasmid is introduced into e.coli cells, from which cells survive in the presence of a specific antibiotic are selected. The selected e.coli cells containing the recombinant plasmid are cultured under conditions that facilitate the expression of the gene of interest. A N-terminal 6xHis tag is linked to the protein. After expression, affinity purification is used to isolate and purify the recombinant Human FGFR1 protein from the cell lysate. Denaturing SDS-PAGE is employed to resolve the resulting recombinant Human FGFR1 protein, revealing a purity greater than 85%.

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Target Background

Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (GnRH) neuronal system. Phosphorylates PLCG1, FRS2, GAB1 and SHB. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Promotes phosphorylation of SHC1, STAT1 and PTPN11/SHP2. In the nucleus, enhances RPS6KA1 and CREB1 activity and contributes to the regulation of transcription. FGFR1 signaling is down-regulated by IL17RD/SEF, and by FGFR1 ubiquitination, internalization and degradation.
Gene References into Functions
  1. myeloid/lymphoid neoplasms with FGFR1 rearrangement are a rare entity, with no distinct clinical phenotype. FGFR rearrangement confirmation by FISH should be performed in any hematological malignancy with 8p translocation. PMID: 29119847
  2. CCND1 , C-MYC , and FGFR1 amplifications were observed in 34.28%, 28.57%, and 17.14% of the 35 samples (invasive ductal breast carcinoma). PMID: 30119151
  3. High FGFR1 expression is associated with Peritoneal Dissemination Via Epithelial-to-Mesenchymal Transition in Gastric Cancer. PMID: 29976636
  4. The present study aimed to evaluate the relationship between a common FGFR1 single nucleotide polymorphism (rs13317) with craniofacial morphology. PMID: 29872111
  5. Clinical outcomes of myeloid/lymphoid neoplasms with fibroblast growth factor receptor-1 (FGFR1) rearrangement PMID: 29486661
  6. Suggest that genomic alterations involving the cell cycle (TP53, CCND1, CDKN2A), as well as FGFR1 amplifications and tumour genomic alterations burden are prognostic biomarkers of survival in head and neck squamous cell carcinoma. PMID: 29331751
  7. novel heterozygous frameshift mutation c.299_300insCCGCAGACTCCGGCCTCTATGC (p.C101Rfs*17) associated with Kallmann syndrome PMID: 29658329
  8. FGFR3, as well as its downstream regulatory PI3K/AKT kinases, may serve as potential biomarkers for the invasiveness and prognosis of laryngeal cancer. PMID: 29299828
  9. Our experiments presented a new mechanism adopted by GDNF supporting glioma development and indicated a possible therapeutic potential via the inhibition of proN-cadherin/FGFR1 interaction. PMID: 29750313
  10. There was no significant difference in the expression of FGFR1 between different types of circulating tumor cells. PMID: 29764586
  11. Our data may facilitate design of therapeutically relevant targeting molecules for selective treatment of FGFR1 overproducing cancers PMID: 29748524
  12. Study finds infrequent BRAF alterations but enriched FGFR alterations in adults as compared with that reported in pediatric pilocytic astrocytomas. In addition, coexistent BRAF and FGFR alterations and a significant association of FGFR alterations with age and tumor location were noted. PMID: 27608415
  13. SNP rs17182023 was correlated to reduced breast cancer risk, and was associated with FGFR1 protein expression. High FGFR1 protein expression was an independent risk factor of breast cancer, and resulted in poor prognosis. PMID: 29996114
  14. Besides RET and HRAS, FGFR1 is only the third protooncogene found to be recurrently mutated in pheochromocytomas. PMID: 29159601
  15. For the treatment of patients with breast cancer and FGFR1 amplifications. PMID: 29223982
  16. presentation of the atomic structure of a 1:1:1 ternary complex that consists of the shed extracellular domain of alpha-klotho, the FGFR1c ligand-binding domain, and FGF23; in this complex, alpha-klotho simultaneously tethers FGFR1c by its D3 domain and FGF23 by its C-terminal tail, thus implementing FGF23-FGFR1c proximity and conferring stability PMID: 29342138
  17. Study identified FGFR1, a promoter of glycolysis-related enzyme, as the target of miR-361 that promoted glycolysis and repressed oxidative phosphorylation in breast cancer cells. FGFR1 mediated the anti-glycolytic function of miR-361 by regulating the activity of PDHK1 and LDHA. PMID: 29132384
  18. FGFR1 and/or FGF3 gene amplification correlated with a lower pathologic complete response in patients with HER2(+) early breast cancer treated with neoadjuvant anti-HER2 therapy. PMID: 28381415
  19. Data demonstrated that FOXC1 binds to an Fgfr1 upstream regulatory region and that FOXC1 activates an Fgfr1 promoter element. Furthermore, elevated expression of Foxc1 led to increased Fgfr1-IIIc transcript promoting invasion after TGFbeta1-induced EMT. PMID: 28684636
  20. These results suggest that FGFR1 gene amplification is a frequent alteration in squamous cell carcinoma of the lung and appears not to be a negative but rather a favorable prognostic marker for women and particularly for patients with advanced disease PMID: 29270870
  21. These data suggest the ERalpha pathway remains active in estrogen-deprived ER(+)/FGFR1-amplified breast cancers. Therefore, these tumors are endocrine resistant and should be candidates for treatment with combinations of ER and FGFR antagonists. PMID: 28751448
  22. Amplification of gene FGFR1 is associated with lung adenocarcinoma. PMID: 28381877
  23. Lysosomal sequestration - resulting in an organelle-specific and pH-dependent nintedanib fluorescence - was identified as an intrinsic resistance mechanism in FGFR-driven lung cancer cells. Accordingly, combination of nintedanib with agents compromising lysosomal acidification (bafilomycin A1, chloroquine) exerted distinctly synergistic growth inhibitory effects PMID: 28882160
  24. the close proximity between AcSDKP and FGFR1 was essential for the suppression of TGFbeta/smad signaling and EndMT associated with MAP4K4 phosphorylation (P-MAP4K4) in endothelial cells. PMID: 28771231
  25. This study reports a highly specific internalizing antibody fragment that can serve as a therapeutic targeting agent for efficient delivery of cytotoxic drugs into FGFR1-positive lung cancer cells. PMID: 28483948
  26. anlotinib inhibits the activation of VEGFR2, PDGFRbeta and FGFR1 as well their common downstream ERK signaling PMID: 29454091
  27. Missense mutations in COL6A1, COL11A2, FGFR1, and BMP2 genetically predispose patients to ossification of posterior longitudinal ligaments. PMID: 27246988
  28. High levels of FGFR1 is associated with non-small cell lung cancer. PMID: 28558758
  29. The results of this study designate nFGFR1 signaling as a potential common dysregulated mechanism in investigated patients and potential therapeutic target in schizophrenia. PMID: 28094170
  30. Findings indicate the great variability of fibroblast growth factor receptor 1 (FGFR1) mutation phenotypes in idiopathic hypogonadotropic hypogonadism (IHH) or Kallmann syndrome (KS). PMID: 28008864
  31. these results show that FGFR1 polymorphism influences lower anterior face height, the distance from the upper lip to the nasal floor, and lip shape PMID: 28415752
  32. Fibrolamellar carcinomas show polysomy of chromosome 8 and the FGFR1 locus, and only modest mRNA expression and weak or absent expression at the protein level. FGFR2 rearrangement was not detected. PMID: 26259677
  33. endothelin-A receptor-activated ABCB1 expression has a role in nintedanib resistance in FGFR1-driven small cell lung cancer PMID: 27367030
  34. Loss of FGFR1 does generate a gene signature that is reverse correlated with FGFR1 gene amplification and/or upregulation in human breast cancer. Our results suggest that FGFR1 signaling is a key pathway driving breast cancer lung metastasis and that targeting FGFR1 in breast cancer is an exciting approach to inhibit metastasis. PMID: 28433771
  35. Combination treatment with AKT and FGFR kinase inhibitors have additive effects on malignant phenotypes in vitro and in vivo by inhibiting multiple signaling pathways and mitigating the compensatory upregulation of FGFR signaling induced by AKT kinase inhibition. PMID: 28008155
  36. FGFR1/MAPK may be important for brachyury activation in lung cancer, and this pathway may be an appealing therapeutic target for a subset of brachyury-driven lung cancer. PMID: 27893433
  37. FGFR1 alteration mainly represented by FGFR1-ITD is a frequent event in dysembryoplastic neuroepithelial tumors. Digital droplet PCRtrade mark is an easy and alternative method than whole-genome sequencing to detect FGFR1-ITD in Formalin-fixed paraffin-embedded brain tumors, in routine practice. PMID: 27791984
  38. Report dramatic upregulation of fibroblast growth factor receptor 1 (FGFR1) and its cognate ligand FGF2 in both acquired and inherently resistant breast cancer cells. PMID: 27825137
  39. This study reveals a stringent association between FGFR and the downstream effector c-Myc in FGFR-dependent cancers, and suggests the potential therapeutic value of c-Myc in FGFR-targeted cancer therapy. PMID: 27401245
  40. Elevated FGFR3 and FGFR1 protein expression is common in aggressive ependymomas but likely not driven by genetic alterations. Further studies are warranted to evaluate whether ependymoma patients with high FGFR3 and/or FGFR1 expression could benefit from treatment with FGFR inhibitor based therapeutic approaches currently under evaluation in clinical trials PMID: 28468611
  41. These data identify FGFR1 as a driver gene in multiple soft-tissue sarcoma subtypes and support FGFR1 inhibition, guided by patient selection according to the FGFR1 expression and monitoring of MAPK-ERK1/2 signaling, as a therapeutic option in this challenging group of diseases PMID: 27535980
  42. Our results demonstrated that the AcSDKP-FGFR1 signaling pathway is critical for maintaining mitochondrial dynamics by control of miR let-7b-5p in endothelial cells. PMID: 29269295
  43. increased FGFR1 CN was observed in two racial groups not previously reported: African Americans and Native Americans. However, FGFR1 amplification is not prognostic in laryngeal squamous cell carcinomas PMID: 29351293
  44. This brief communication reports on a patient with an exceedingly rare "8p11 (eight-p-eleven) myeloproliferative syndrome" (EMS) with CEP110-FGFR1 rearrangement who responded to treatment with the multi-tyrosine kinase inhibitor (TKI) dasatinib PMID: 28242791
  45. Identify mutually exclusive activating hotspot mutations in FGFR1 and related PI-3K/RAS signaling genes in malignant phyllodes tumors which are implicated in tumor pathogenesis and/or progression. PMID: 27255162
  46. we report FGFR1 as being frequently overexpressed in HNSCC and as a candidate prognostic biomarker in HPV-negative HNSCC. PMID: 26936917
  47. Head and neck cancers are recurrently affected by FGFR1 amplification, with a predominance in cancers of the oral cavity. PMID: 29022097
  48. High FGFR1 expression is associated with non-small cell lung cancer. PMID: 26936993
  49. Study present a rare case of a 46,XY patient with CHD associated with ambiguous genitalia consisting of a clitoris-like phallus and a bifid scrotum. Exome sequencing revealed novel homozygous mutations in the FGFR1 and STARD3 genes that may be associated with the phenotype. PMID: 27055092
  50. PDGFRalpha levels are regulated by SMARCB1 expression, and assessment of clinical specimens documents the expression of both PDGFRalpha and FGFR1 in rhabdoid tumor patients. PMID: 27783942

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Involvement in disease
Pfeiffer syndrome (PS); Hypogonadotropic hypogonadism 2 with or without anosmia (HH2); Osteoglophonic dysplasia (OGD); Hartsfield syndrome (HRTFDS); Trigonocephaly 1 (TRIGNO1); Encephalocraniocutaneous lipomatosis (ECCL); Jackson-Weiss syndrome (JWS)
Subcellular Location
Cell membrane; Single-pass type I membrane protein. Nucleus. Cytoplasm, cytosol. Cytoplasmic vesicle. Note=After ligand binding, both receptor and ligand are rapidly internalized. Can translocate to the nucleus after internalization, or by translocation from the endoplasmic reticulum or Golgi apparatus to the cytosol, and from there to the nucleus.
Protein Families
Protein kinase superfamily, Tyr protein kinase family, Fibroblast growth factor receptor subfamily
Tissue Specificity
Detected in astrocytoma, neuroblastoma and adrenal cortex cell lines. Some isoforms are detected in foreskin fibroblast cell lines, however isoform 17, isoform 18 and isoform 19 are not detected in these cells.
Database Links

HGNC: 3688

OMIM: 101600

KEGG: hsa:2260

STRING: 9606.ENSP00000393312

UniGene: Hs.264887

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