STI-6643
Based on 1 Customer Validation
STI-6643 is a fully human IgG4 antibody that targets CD47. STI-6643 blocks CD47-SIRPα interaction, and enables macrophage-mediated phagocytosis of tumor cells. STI-6643 shows anti-tumor activity in mouse lymphoma xenograft models. STI-6643 can be used for the research of Burkitt's lymphoma, solid tumors, relapsed or refractory tumors, and lymphoma. The isotype control for STI-6643 can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).
For research use only. We do not sell to patients.
- Purity : 99.62%
- CAS No.: 2376730-61-7
- Molecular Weight:143.875 kDa
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Storage:Shipping with dry ice
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Isotype
Human IgG4 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
CD47
In Vitro
STI-6643 binds to human CD47 with a Kd of 76 nM, with lower affinity for cynomolgus (177 nM) and canine (134 nM) CD47 antigens[1].
STI-6643 (25 min) binds dose-dependently to human MDA-MB-231 (EC50 ~30.0 µg/mL), human RAJI (EC50 6.64 µg/mL), canine OSCA-40 (EC50 ~30.0 µg/mL), and canine OSCA-78 (EC50 ~30.0 µg/mL) cancer cells[1].
STI-6643 (0.09-200 µg/mL; 15 min) dose-dependently blocks the CD47/SIRPα interaction on human CCRF-CEM cells with an IC50 of 3.65 µg/mL, without reaching saturation at concentrations up to 200 µg/mL[1].
STI-6643 (0.0001-10 µg/mL; 30 min) enhances macrophage-mediated phagocytosis of human RAJI-GFP cells[1].
STI-6643 (1.5625-50 µg/mL) does not exhibit direct tumor cell killing activity on human CCRF-CEM leukemia cells[1].
STI-6643 (100 µg/mL; 25 min) exhibits negligible binding to human (EC50 = 11.76 µg/mL) and cynomolgus monkey (EC50 = 20.32 µg/mL) RBCs, with slightly stronger binding to canine RBCs (EC50 = 5.10 µg/mL)[1].
STI-6643 (0.001-300 µg/mL; 20 h) does not induce hemagglutination of human or cynomolgus monkey RBCs at concentrations up to 300 µg/mL, and exhibits weak, 100-fold less potent hemagglutination activity than Hu5F9 in canine RBCs[1].
STI-6643 (0.001-100 µg/mL; 3 days) preserves human T cell survival and functionality in a superantigen stimulation assay, with minimal impact on IFN-γ secretion[1].
STI-6643 (0.001-500 µg/mL; 6 days) preserves the survival of human CD4+, CD8+, CD19+, and CD56+ immune cells[1].
STI-6643 (2.5-5 ng/mL; 30 min) in combination with Rituximab (HY-P9913) enhances macrophage-mediated phagocytosis of human RAJI-GFP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
STI-6643 (20 mg/kg; i.v.; 3x/week; 2 consecutive weeks) in combination with Rituximab enhances anti-tumor activity and survival in a mouse disseminated Burkitt's lymphoma xenograft model[1].
STI-6643 (10 mg/kg; s.c.; 6 doses on days 6, 8, 10, 13, 15 and 17) preserves functional human T cells in a mouse xenograft GVHD model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fox Chase/SCID mice (6-8 weeks old) intravenously injected with RAJI-Fluc cells[1]
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Dosage:0.1; 1; 10; 30; 60 mg/kg
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Administration:i.v.; 3x/week; 2 consecutive weeks
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Result:Reduced systemic tumor bioluminescence flux to levels comparable to Hu5F9 at 30 mg/kg.
Produced a 73% survival rate at 30 mg/kg.
Maintained healthy body weights in most animals at 30 mg/kg.
Significantly inhibited systemic tumor expansion and prolonged survival at 10 mg/kg.
Produced significant anti-tumor activity and survival in less aggressive tumor growth conditions at 1 mg/kg.
Showed no significant anti-tumor activity in more aggressive tumor growth conditions at 0.1 mg/kg.
Significantly prolonged survival at 60 mg/kg.
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Animal Model:Fox Chase/SCID mice (6-8 weeks old) intravenously injected with RAJI-Fluc cells[1]
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Dosage:20 mg/kg
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Administration:i.v.; 3x/week; 2 consecutive weeks
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Result:Showed improved anti-tumor activity compared to either monotherapy when combined with rituximab.
Achieved an 88% endpoint survival rate.
Caused no adverse events or toxicity during the study.
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Animal Model:NSG-Tg (hIL-15) mice (6-8 weeks old) intraperitonealy injected with human PBMCs on day -6, and subcutaneously injected with MDA-MB-231 cells on day 0[1]
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Dosage:10 mg/kg
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Administration:s.c.; 6 doses on days 6, 8, 10, 13, 15 and 17
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Result:Caused a ~50% decrease in circulating CD3+ T cells compared to isotype control.
Re-established a physiological CD4:CD8 ratio of 2:1.
Did not alter GVHD development kinetics .
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Gene ID
Accession
Q08722-1
Conjugated
Unconjugated
Reconstitution
The product can be reconstituted/diluted with sterile PBS or saline.
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized CD47 Protein, Human (HEK293, HY-P72917) can bind STI-6643. The EC50 for this effect is 161.5 ng/mL.
Chemical Information
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CAS No. 2376730-61-7
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Appearance Liquid
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Molecular Weight 143.875 kDa
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Color Colorless to light yellow
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SMILES
[STI-6643]
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (263 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
[1]. Thaker YR, et al. A Novel Affinity Engineered Anti-CD47 Antibody With Improved Therapeutic Index That Preserves Erythrocytes and Normal Immune Cells. Front Oncol. 2022;12:884196. Published 2022 May 19. [Content Brief]
[2]. Xu S, et al. Targeting immune checkpoints on tumor-associated macrophages in tumor immunotherapy. Front Immunol. 2023 May 29;14:1199631. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)