IMC-D11
Based on 1 Customer Validation
IMC-D11 (LY-3076226 antibody) is an anti-FGFR3 IgG1 monoclonal antibody with an EC50 of approximately 0.1 nM against hFGFR3b and hFGFR3c. IMC-D11 inhibits the growth of FGFR3-dependent lung adenocarcinoma in mouse models and shows no effect on tumors that do not express FGFR3. IMC-D11 can serve as an ADC Antibody for ADC synthesis, such as LY3076226. IMC-D11 is applicable to research related to urothelial carcinoma, multiple myeloma, lung adenocarcinoma, as well as advanced or metastatic cancers.
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- Purity: 98.51%
- 분자량:145.82 kDa
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
Human IgG1 kappa
Human
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FGFR3 ~0.1 nM (EC50) |
IMC-D11 binds to hFGFR3b and hFGFR3c with an EC50 of approximately 0.1 nM, and exhibits extremely low binding affinity for other FGFR family members[2].
IMC-D11 binds to FGFR3b and FGFR3c expressed on the surface of BaF3 cells, but does not bind to parental BaF3 cells[2].
IMC-D11 (preincubated for 1 h, total duration 72 h) inhibits FGF1- and FGF9-dependent viability in BaF3 cells expressing FGFR3b and FGFR3c, with IC50 values ranging from 1.6 to 41.3 nM[2].
IMC-D11 (0.09-200 nM; 72 h) induces a dose-dependent decrease in FGFR3 protein in UMUC-14 bladder cancer cells after 72 h of incubation[2].
IMC-D11 (up to 200 nM; 72 h) inhibits the proliferation of UMUC-14 bladder cancer cells carrying the FGFR3S249C mutation in a dose-dependent manner[2].
IMC-D11 potently blocks ligand-dependent signaling pathways of FGFR3 in tumor cells, promotes receptor internalization, and delivers targeted cytotoxins to FGFR3-activated cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BaF3 cells stably expressing human FGFR3b, BaF3 cells stably expressing human FGFR3c
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Concentration:Serial dilutions; 3.7 nM FGF1; 3.7 nM FGF9; 15 µg/mL heparin
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Incubation Time:1 h (pre-incubation); 72 h (total)
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Result:Inhibited the mitogenic response of FGFR3-expressing BaF3 cells to FGF1 or FGF9 with an IC50 ranging from 1.6 to 41.3 nM.
Had no detectable agonist activity.
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Cell Line:UMUC-14 bladder carcinoma cells (harboring constitutively active FGFR3^S249C)
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Concentration:Serial dilutions up to 200 nM
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Incubation Time:72 h
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Result:Significantly inhibited UMUC-14 cell growth in a dose-dependent manner compared to human IgG control.
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Cell Line:UMUC-14 bladder carcinoma cells
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Concentration:0.09-200 nM
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Incubation Time:72 h
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Result:Caused dose-dependent loss of FGFR3 protein, likely through internalization and degradation.
Reduced FGFR3/α-tubulin band intensity observed at all tested concentrations relative to human IgG control.
| Species | Dose | Route | Plasma Concentration |
|---|---|---|---|
| Mice[2] | 40 mg/kg | i.p. | 1124 μg/mL |
IMC-D11 (40 mg/kg; i.p.; two doses 15 hours apart) significantly reduces FGFR3-dependent proliferation of Sftpc+/CC10+ bronchioalveolar duct junction cells in FVB mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:FVB (6-12 weeks old; doxycycline-induced FGFR3-dependent tumorigenesis)[2]
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Dosage:40 mg/kg
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Administration:i.p.; every 2 days; 16 days
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Result:Prevented tumor-associated weight loss, with treated mice gaining an average of 0.5 g over the experimental period.
Achieved mean plasma levels of 1124 µg/mL 24 hours after the last injection.
Reduced average lung pathology score to 1.8, a significant reduction from the control score of 3.8 (P<0.0001).
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Animal Model:FVB (6-12 weeks old; doxycycline-induced FGFR3-dependent epithelial proliferation)[2]
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Dosage:40 mg/kg
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Administration:i.p.; two doses 15 hours apart
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Result:Did not affect the number of Sftpc+/CC10+ cells in the bronchioalveolar duct junction region.
Caused a significant (P<0.002) decrease in the ratio of PCNA-positive (proliferating) cells to Sftpc+/CC10+ cells compared to untreated controls.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
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Immobilized Human FGFR3 Protein (ECD, alpha IIIb, His Tag) can bind IMC-D11. The EC50 for this effect is 60.8 ng/mL.
Chemical Information
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Appearance Liquid
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분자량 145.82 kDa
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Color Colorless to light yellow
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SMILES
N/A
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Synonyms
LY-3076226 antibody
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선적
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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Data Sheet (266 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
[2]. Yin Y, et al. Inhibition of fibroblast growth factor receptor 3-dependent lung adenocarcinoma with a human monoclonal antibody. Disease models & mechanisms. 2016 May 01;9(5):563-71. [Content Brief]
[3]. Kollmannsberger C, et al. A phase 1 study of LY3076226, a fibroblast growth factor receptor 3 (FGFR3) antibody-drug conjugate, in patients with advanced or metastatic cancer. Invest New Drugs. 2021 Dec;39(6):1613-1623. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IMC-D11 Related Classifications
HY-P991106 Related Classifications
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