Tigilanol tiglate  (Synonyms: EBC-46)

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^[1][2][3].

Tigilanol tiglate (300-500 µM, 1-12 h) 促进癌细胞 MM649 和 A-431 中损伤相关分子模式的释放/外化^[1]。
Tigilanol tiglate (1 µg/mL, 10 min-24 h) 诱导分泌组谱的变化，从而改变 H357 头颈癌细胞中的 c-met 磷酸化和细胞表面蛋白表达^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tigilanol tiglate (66.5-533 μM，50 μL，瘤内注射) 以浓度依赖性方式快速消融 BALB/c Foxn1^nu 裸鼠中的黑色素瘤异种移植肿瘤^[1]。
Tigilanol tiglate (1 mg/mL，每 cm³ 肿瘤体积 0.5 mL，瘤内注射) 对改善狗肥大细胞肿瘤非常有效^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

562.65

C₃₀H₄₂O₁₀

943001-56-7

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [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]