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:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Human IgG4 kappa
Human
CD47
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.
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 .
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Q08722-1
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
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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)
- 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)
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