INCA033989
INCA033989 is a fully human IgG1 monoclonal antibody targeting mutCALR (KD = 1.75 nM for mutCALRdel52; KD = 6.78 nM for mutCALRins5). INCA033989 antagonizes mutCALR-driven signaling and proliferation. INCA033989 selectively inhibits pSTAT3/pSTAT5. INCA033989 prevents thrombocytosis and reduces the expansion of mutCALR-positive cells. INCA033989 is useful for research on myeloproliferative neoplasms .
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Human
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STAT3 |
STAT5 |
INCA033989 binds to recombinant mutCALRdel52 and mutCALRins5 proteins with nanomolar affinities (KD = 1.75 nM for mutCALRdel52; 6.78 nM for mutCALRins5), showing slight preferential binding to mutCALRdel52[1].
INCA033989 (72 h) selectively inhibits cytokine-independent proliferation of Ba/F3-TPOR/CALRdel52 and UT-7-TPOR/CALRdel52 cells (IC50 = 0.1 μg/mL; IC90 = 1 μg/mL)[1].
INCA033989 (4 h) broadly inhibits mutCALR-driven oncogenic signaling (including pSTAT5) in Ba/F3-TPOR/CALRdel52 cells[1].
INCA033989 (4 h) does not induce complement-dependent cytotoxicity in TF-1-TPOR/CALRdel52 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
INCA033989 (3-10 mg/kg; i.p.; twice weekly; 10 weeks) prevents thrombocytosis, reduces mutCALR-positive cell expansion, and normalizes bone marrow histology in C57BL/6 (CD45.2+; lethally irradiated recipients), CD45.2+ floxed homozygous CALRdel52 KI, CD45.2+ wt transgenic (UBI-GFP/BL6) mice model of Myeloproliferative neoplasm [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD scid gamma (NSG)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Decreased numbers of Ba/F3 cells in the blood, reduced spleen weight compared to isotype control, and achieved a plasma concentration of 50 μg/mL on day 13
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Animal Model:C57BL/6 (CD45.2+; lethally irradiated recipients); CD45.2+ floxed homozygous CALRdel52 KI; CD45.2+ wt transgenic (UBI-GFP/BL6)[1]
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Dosage:3-10 mg/kg
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Administration:i.p.; twice weekly; 10 weeks
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Result:Prevented thrombocytosis with platelet counts remaining within normal range, inhibited expansion of mutCALR-positive platelets (36% vs 96% in isotype control), reduced mutCALR-positive long-term hematopoietic stem cells (32% vs 85% in isotype control), and normalized bone marrow histology with normal megakaryocyte numbers
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
P27797
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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Appearance Liquid
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Color Colorless to light yellow
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Envío
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Ficha de datos (262 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)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
INCA033989 Related Classifications
HY-P991888 Related Classifications
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- INCA033989
- INCA 033989
- INCA-033989
- STAT
- UT-7-TPOR/CALRdel52
- mutated calreticulin
- disease-initiating cells
- mutCALR
- MPN
- dynamin-mediated endocytosis
- floxed homozygous CALRdel52 KI
- megakaryocyte
- TF-1-TPOR/CALRdel52
- JAK2V617F-positive cells
- mutCALRdel52
- hematopoiesis
- Ba/F3-TPOR/CALRdel52
- bone marrow
- UBI-GFP/BL6
- lysosomal degradation
- mutCALRins5
- Ba/F3-EPOR/JAK2V617F
- pSTAT5
- NOD scid gamma (NSG) mice
- myeloproliferative neoplasms
- primary CD34+ cells
- C57BL/6
- primary CD34? HSPCs
- TPOR
- thrombocytosis
- CD45.2+
- Inhibitor
- inhibitor
- inhibit