IMC-EB10
Based on 1 Customer Validation
IMC-EB10 (LY3012218) is an anti-FLT3 monoclonal antibody. IMC-EB10 binds to FLT3 with high affinity (Kd = 158 pM) and blocks the binding of FLT3 ligand to FLT3 (IC50 ≈ 10 nM), thereby inhibiting MAPK, STAT5, and PI3K/Akt signaling in leukemia cells. IMC-EB10 can enhance the anti-leukemic effect of Methotrexate (HY-14519) and inhibit leukemias expressing wild-type or ITD-mutated FLT3 receptors. IMC-EB10 prolongs the survival of acute lymphoblastic leukemia (ALL) cells and primary leukemia samples and reduces engraftment in non-obese diabetic/severe combined immunodeficiency patients. IMC-EB10 is indicated for leukemia research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98%
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Speicherung:
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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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
Isotype
Human IgG1 kappa
Recommend Isotype Controls
Species Reactivity
Human
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STAT5 |
In Vitro
IMC-EB10 (10 μg/mL, 1 h) reduces FLT3 and phosphorylation of downstream signaling proteins STAT5, Akt, and MAPK in Hb1119 and SEM-K2 cells, but activates them in REH and RS411 cells[1].
IMC-EB10 (10 μg/mL, 1 h) activates FLT3 and downstream Akt in ALLs[1].
IMC-EB10 (0.4-200 nM, 1 h) inhibits FLT3-Fc-induced phosphorylation of wild-type FLT3 and ligand-independent constitutive phosphorylation of ITD-mutant FLT3 in EOL-1, EM3, BaF3-ITD and MV4;11 cells[4].
IMC-EB10 (0.4-200 nM, 1 h) inhibits FLT3-Fc-induced phosphorylation of MAPK, AKT and Stat5 in EOL-1, EM3, BaF3-ITD and MV4;11 cells[4].
IMC-EB10 (1.5-100 nM, 1 h) inhibits proliferation of FLT3-Fc-induced proliferation of EOL-1 and BaF3-ITD cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Hb1119, SEM-K2 cells
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Concentration:10 μg/mL
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Incubation Time:1 h
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Result:Reduced FLT3 and phosphorylation of downstream signaling proteins STAT5, Akt, and MAPK.
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Cell Line:REH, RS411 cells
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Concentration:10 μg/mL
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Incubation Time:1 h
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Result:Activated FLT3 and phosphorylation of downstream signaling proteins STAT5, Akt, and MAPK.
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Cell Line:ALLs
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Concentration:10 μg/mL
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Incubation Time:1 h
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Result:Activated FLT3 and downstream Akt.
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Cell Line:EOL-1, EM3, BaF3-ITD, MV4;11 cells
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Concentration:0.1, 0.4, 1, 4, 10, 40, 100, 200 nM
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Incubation Time:1 h
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Result:Blocked FL-induced FLT3 receptor phosphorylation in a dose dependent manner with an IC50 of 0.4 to 4 nM.
Blocked the phosphorylation and constitutive phosphorylation of MAPK, inhibited FL-induced phosphorylation of AKT and Stat5 phosphorylation in EOL-1 and BaF3-ITD cells.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-inf |
|---|---|---|---|---|
| Mice[2] | 20 mg/kg | i.p. | 96 h | 38327 μg·h/mL |
In Vivo
IMC-EB10 (400 μg, i.p., three times a week, 14 weeks) reduces cell implantation in ALLs NOD/SCID mice model[1].
IMC-EB10 (100-500 μg, i.p., 3 times weekly, 20 days) decreases the number of tumor cells in bone marrow and prolongs the survival in EOL-1 and BaF3-ITD xenograft leukemia model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SEM-K2 (0.5×106) NOD/SCID mice model[1]
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Dosage:400 μg
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Administration:i.p., thrice per week starting 24 hours after cell injection/once starting 24 hours after cell injection/a total of thrice every other day starting 24 hours after cell injection or thrice per week starting 7 days after cell injection, 30 days
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Result:Reduced human cells in peripheral blood, spleen, and bone marrow, reducing the presence of SEM-K2 cells to <1%, prolonged survival.
Did not select for resistant cells, mediated cytotoxicity through natural killer cells.
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Animal Model:ALLs (1×106) NOD/SCID mice model[1]
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Dosage:400 μg
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Administration:i.p., three times a week, 14 weeks
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Result:Reduced cell implantation.
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Animal Model:SEM-K2 (5×105) NOD/SCID mice model[3]
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Dosage:10 mg/kg + 100 mg/kg Methotrexate
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Administration:i.p., 2×/week, 3 weeks + once per week for 3 weeks
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Result:Significantly prolonged survival compared to Methotrexate alone.
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Animal Model:EOL-1 (5×106) xenograft leukemia NOD/SCID mice (male, , 6-8 weeks) model[4]
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Dosage:100, 250, 500 μg
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Administration:i.p., 3 times weekly, 20 days
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Result:Decreased the number of tumor cells in bone marrow.
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Animal Model:BaF3-ITD (5×104) xenograft leukemia NOD/SCID mice (male, , 6-8 weeks) model[4]
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Dosage:100, 500 μg
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Administration:i.p., 3 times weekly
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Result:Prolonged the survival.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Anwendung
ELISA, FACS, Functional assay
Verified Bioactivity
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Loaded IMC-EB10 on ACH2 biosensor, can bind HY-P75183 FLT3 Protein, Human (T227M, HEK293, His) with an affinity constant of 4.903E-07 M as determined in BLI assay.
Chemical Information
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
N/A
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Synonyms
LY3012218
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Versand
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (268 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)
Verweise
[1]. Piloto O, et al. IMC-EB10, an anti-FLT3 monoclonal antibody, prolongs survival and reduces nonobese diabetic/severe combined immunodeficient engraftment of some acute lymphoblastic leukemia cell lines and primary leukemic samples. Cancer Res. 2006 May 1;66(9):4843-51 [Content Brief]
[4]. Li Y, et al. Suppression of leukemia expressing wild-type or ITD-mutant FLT3 receptor by a fully human anti-FLT3 neutralizing antibody. Blood.2004 Aug 15;104(4):1137-44. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
IMC-EB10 Related Classifications
HY-P991641 Related Classifications
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