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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Human IgG1 kappa
Human
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STAT5 |
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.
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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.
| Species | Dose | Route | T1/2 | AUC0-inf |
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| Mice[2] | 20 mg/kg | i.p. | 96 h | 38327 μg·h/mL |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
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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.
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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