Home Biosimilar Antibodies Angiogenesis VEGFR inhibitor Ramucirumab (anti-VEGFR2)
For research use only. Not for use in humans.

Ramucirumab (anti-VEGFR2)

Synonyms: IMC-1121B, LY3009806, IMC-1121

Ramucirumab is a monoclonal antibody of the IgG1 class that binds to VEGF-R2 and prevents its activation. The IC50 value for blocking KDR binding to VEGF is 0.8 nM for ramucirumab, MW: 143.6 KD.

Ramucirumab (anti-VEGFR2)

Click to purchase the isotype control of Ramucirumab (anti-VEGFR2)

3 Citations

The Nobel Prize

17 Nobel Prize winners have used Selleck products

Shimon Sakaguchi

Nature Communications 2025,16, Article number:1325

David Baker

Dev Cell 2023, 58(20):2163-2180.e9.

David Julius

Cell 2017, 185-198.e16

Michael Houghton

Cell Chem Biol, 2020, 27(7):780-792.e5

Charles M. Rice

Cell 2018, 172(3):423-438.e25

Quality Control

Batch: Purity: 99.4% Protein concentration: 5mg/ml Endotoxin Level: ≤1 EU/mg
99.4

Specificity

Name Citation VEGFR1 VEGFR2 VEGFR3 VEGFR VEGF Others
Foretinib 94 Met,Tie-2,RON
Cediranib (AZD2171) 67 c-Kit,PDGFRβ,FGFR1
PD173074 124 FGFR1
Dovitinib (TKI-258) 52 FLT3,c-Kit,FGFR1
Linifanib (ABT-869) 33 CSF-1R,FLT3,Kit
Vatalanib (PTK787) 2HCl 53 PDGFRβ,c-Kit,c-Fms
RAF265 (CHIR-265) 24 B-Raf
Motesanib Diphosphate (AMG-706) 12 Kit,RET,PDGFR
Brivanib (BMS-540215) 10 FGFR1
MGCD-265 analog 12 Met,RON,Tie-2
AEE788 (NVP-AEE788) 13 EGFR,HER2/ErbB2,c-Abl
ENMD-2076 9 FLT3,RET,Aurora A
OSI-930 7 CSF-1R,LCK,C-Raf
CYC116 10 Aurora A,Aurora B,FLT3
Ki8751 21 c-Kit,PDGFRα
Telatinib 5 c-Kit,PDGFRα
PP121 5 PDGFR,Hck,mTOR
KRN 633 6 PDGFRα,c-Kit,BTK
SAR131675 34
Apatinib (YN968D1) mesylate 26 RET
BMS-794833 2 Met
Brivanib Alaninate (BMS-582664) 2 FGFR1
Golvatinib (E7050) 8 c-Met
Semaxanib (SU5416) 21
ZM 323881 HCl 20
ZM 306416 13 Src,Abl
R1530 0 FGFR1
Chiauranib 0 c-Kit,CSF-1R,Aurora B
Emvododstat (PTC299) 0 Dihydroorotate dehydrogenase
XL092 0 AXL,MER,MET
Lucitanib (E3810) hydrochloride 1 FGFR1,FGFR2
Ningetinib 0 Axl,c-Met
Ki20227 1 c-Fms,PDGFRβ,c-Kit
Tyrphostin AG1433 0 PDGFRβ
SU14813 2 PDGFRβ,KIT
Sulfatinib 1 CSF1R,FGFR1
CS-2660 (JNJ-38158471) 0 RET,Kit
SU5204 1 HER2
SU5214 0 EGFR
SU5205 0
SU5408 2
Pamufetinib (TAS-115) 0 recombinant MET
ODM-203 0 FGFR3,FGFR1,FGFR2
WHI-P180 0 RET
Altiratinib 3 MET Y1230C,TrkA,TrkC
Motesanib (AMG-706) 11 c-Kit,c-Ret,PDGFR
Fruquintinib (HMPL-013) 6
Apatinib 28 RET
Cediranib Maleate 14 c-Kit,PDGFRβ,FGFR1
Toceranib phosphate 1 PDGFR
Anlotinib (AL3818) dihydrochloride 48 c-Kit
Sitravatinib (MGCD516) 7 DDR2,EPHA3,Axl
BFH772 0
BAW2881 (NVP-BAW2881) 3 C-Raf-1,B-RAFV599E,c-Abl
SU5402 24 FGFR1,PDGFRβ
Dovitinib (TKI258) Lactate monohydrate 31 FLT3,c-Kit,FGFR1
LY2874455 15 FGFR2,FGFR1,FGFR4
SKLB1002 5
AZD2932 3 PDGFRβ,Flt3,c-Kit
WAY-340935 0
hVEGF-IN-1 0
4SC-203 0
Chebulinic acid 0
Nastorazepide 0
Vorolanib 0 PDGFR
MAZ51 1 RhoA,GSK3β,Akt
SU5208 0
SU5614 3 FLT3,c-Kit,RET
AG-13958 0
SKLB 610 2 FGFR2,PDGFR
SU1498 2
ZD-4190 0 Flt-1
PDGFR inhibitor 1 4 PDGFR,Kit,c-Fms
Taxifolin (Dihydroquercetin) 4
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1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Mechanism of Action

Description
Ramucirumab is a monoclonal antibody of the IgG1 class that binds to VEGF-R2 and prevents its activation. The IC50 value for blocking KDR binding to VEGF is 0.8 nM for ramucirumab, MW: 143.6 KD.
Targets/IC50/Ki
KDR/VEGF interaction
0.8 nM
In vitro
Ramucirumab is direct inhibitor of VEGF-R2, where it binds to the extracellular VEGF-binding domain with high degree of specificity and affinity, at picomolar dose range. It thus prevents the binding of the VEGF ligand to the VEGF-R2 receptor. Ramucirumab has potential advantages over bevacizumab as it is selective for VEGF-R2, whereas bevacizumab by targeting VEGF-A affects VEGF-R1, -R2, and the noncatalytic coreceptors neuropilin-1and -2. Ramucirumab prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D to its receptors. Thus, ramucirumab inhibits the angiogenesis pathways involved in the development and progression of gastric cancer. ramucirumab demonstrates inhibition of VEGF-stimulated VEGFR-2 activation, proliferation of human endothelial cells, VEGF migration of human leukemia cells, and VEGF induced phosphorylation of VEGFR-2 in human umbilical vein and porcine aortic endothelial cells overexpressing VEGFR-2. Preclinical in vitro data revealed that ramucirumab has a high affinity for VEGFR-2, showing a half-maximal effective concentration (EC50) of 0.15 nM, 8- to 9-fold higher than its natural ligand VEGFA. Ramucirumab binds VEGFR-2 in domain 3 near the N-terminus, both as a soluble protein and as a cell-surface receptor, with a IC50 of 1-2 nM.
Cell Research

The anti-KDR antibodies were added to the microwells of a 96-well plate coated with KDR(Ig1-7) (full-length KDR ECD), KDR(Ig1-3) (variant that contains only the first three N-terminal Ig domains of KDR ECD), or KDR(Ig1) (variant that contains only the first N-terminal Ig domain of KDR ECD) and incubated at room temperature for 1 h. The plate was washed and then incubated with a mouse anti-human Fc antibody-HRP conjugate for additional 1 h, after which the plate was developed as described above. Antibody binding to the two Ig deletion variants are shown as relative (as percentages) to their binding to the full-length KDR ECD.
In vivo
In preclinical studies, ramucirumab concentrations of >20 μg/mL were associated with anticancer activity. And ramucirumab potently inhibited VEGF binding to VEGFR-2 with a binding affinity constant of ramucirumab to VEGFR-2 of 5 × 10-11 M. Pharmacokinetic evaluation has demonstrated a nonlinear pharmacokinetic, with incremental doses of this agent being associated with a decrease in clearance. Ramucirumab has a half-life of 200-300 h. Preclinical studies were also to be conducted in mice, but interspecies receptor differences made ramucirumab inactive in preclinical mouse models.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/27144874/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12917408/

Product Details

CAS No. 947687-13-0
Isotype human IgG1
Sterility 0.2 μM filtered
Formulation PBS buffer, pH 7.2
Storage
(From the date of receipt)		 Store the undiluted solution at 4°C in the dark to avoid freeze-thaw cycles

Comparison of Clones for

*Literature analysis of various clone (for this target) products available on the market shows that Selleck's selected clones are more frequently applied. (data until September 2024)

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