Tigilanol tiglate
Based on 1 Customer Validation
Tigilanol tiglate (EBC-46) is a protein kinase C (PKC)/C1 domain activator. Tigilanol tiglate is associated with mitochondrial/endoplasmic reticulum (ER) dysfunction, leading to activation of the unfolded protein response (UPRmt/ER) and subsequent induction of ATP depletion, organelles expansion, Caspase activation, gasdermin E cleavage, and terminal necrosis. Tigilanol tiglate, as a small anti-tumor molecule with immunomodulatory effects, can be used in the study of head and neck squamous cell carcinoma and soft tissue sarcoma.
For research use only. We do not sell to patients.
- Purity: 96.35%
- CAS No.: 943001-56-7
- Formula: C30H42O10
- Molecular Weight:562.65
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
11.9 nM
Compound: 2a; ebc-46
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Cytotoxicity against PKC sensitive human K562 cells assessed as inhibition of cell growth measured after 7 days by Cell Titer Aqueous96 one solution reagent assay
Cytotoxicity against PKC sensitive human K562 cells assessed as inhibition of cell growth measured after 7 days by Cell Titer Aqueous96 one solution reagent assay
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[PMID: 35973043] |
| Neutrophil | EC50 |
125 nM
Compound: 2a; ebc-46
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Induction of ROS production in human polymorphonuclear neutrophils incubated for 10 mins by DHE staining based fluorescence assay
Induction of ROS production in human polymorphonuclear neutrophils incubated for 10 mins by DHE staining based fluorescence assay
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[PMID: 35973043] |
Tigilanol tiglate (300-500 µM, 1-12 h) promotes the release/externalization of damage associated molecular patterns from cancer cells MM649 and A-431[1].
Tigilanol tiglate (1 µg/mL, 10 min-24 h) induces changes in secretome profiles, which altering c-met phosphorylation and cell surface protein expression in H357 head and neck cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tigilanol tiglate (1 mg/mL, 0.5 mL per cm3 of tumor volume, intratumoral) is highly efficacious for the improvement of mast cell tumors in dogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 943001-56-7
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Appearance Solid
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Molecular Weight 562.65
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Formula C30H42O10
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Color White to off-white
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SMILES
CC[C@H](C)C(O[C@@]12[C@@]([C@]3([H])[C@@]4([H])[C@](O4)([C@H]([C@]5([C@](C=C(C5=O)C)([H])[C@]3([C@@H]([C@H]2OC(/C(C)=C/C)=O)C)O)O)O)CO)([H])C1(C)C)=O
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Synonyms
EBC-46
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Cullen J K, et al. Tigilanol tiglate is an oncolytic small molecule that induces immunogenic cell death and enhances the response of both target and non-injected tumors to immune checkpoint blockade[J]. Journal for ImmunoTherapy of Cancer, 2024, 12(4). [Content Brief]
[2]. Miller J, et al. Dose Characterization of the Investigational Anticancer Drug Tigilanol Tiglate (EBC-46) in the Local Treatment of Canine Mast Cell Tumors. Front Vet Sci. 2019 Apr 9;6:106. [Content Brief]
[3]. Antwi FD, et al. Tigilanol Tiglate-Induced Changes in Secretome Profiles Alter C-Met Phosphorylation and Cell Surface Protein Expression in H357 Head and Neck Cancer Cells. Cells. 2024 Jun 5;13(11):982. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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