Toosendanin

Chemical Structure : Toosendanin

CAS No.: 58812-37-6

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货号: PC-49800Not For Human Use, Lab Use Only.

Toosendanin is a small-molecule compound that blocks macrophage-mediated immunosuppression and activates T cells by inhibiting Hck and Lyn kinases, reprograms macrophages to enforce antitumor immunity in glioblastoma (GBM).

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10 mg	￥580	In stock
25 mg	￥980	In stock
50 mg	￥1580	In stock
100 mg	￥2580	In stock
250 mg		Get quote

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生物&药学活性

Toosendanin is a small-molecule compound that blocks macrophage-mediated immunosuppression and activates T cells by inhibiting Hck and Lyn kinases, reprograms macrophages to enforce antitumor immunity in glioblastoma (GBM).
Toosendanin is a triterpenoid originally extracted from medicinal herb Melia toosendan Sieb that was traditionally used as a parasiticide and insecticide in Eastern medicine.
Toosendanin specificly inhibits IL-10 transcription in tumor-educated macrophages with minimal effects on basal viability in human macrophages, astrocytes, T cells, and glioma cells.
Toosendanin inhibited expression of CD206, a surface marker of immunosuppressive alternatively polarized M2-like macrophages, as well as of IL-10.
Toosendanin (10 nM) almost completely abrogated CD206 and IL-10 expression in Mϕs treated with IL-4 and IL-6, two cytokines known to induce macrophage immunosuppressive polarization.
Toosendanin inhibited in vitro kinase activities of purified Hck and Lyn proteins with KD of 3.2 and 5.9 uM, respectively.
Toosendanin enhanced carboxyfluorescein diacetate succinimidyl ester (CFSE) diffusion into the proliferative T cells, increased CD25+CD3+ activated T cells, and up-regulated expression of effector cytokine interferon-γ (IFN-γ) and proliferative marker Ki67 in CD8+ T cells.
Toosendanin reversed tumor immunosuppression and stimulated antitumor T cell immunity in mouse models of GBM, overcame GBM resistance to immune checkpoint blockade and sensitizes GBM tumors to CAR T immunotherapy in mice.
Toosendanin exhibited efficacy against Mϕ-mediated immunosuppression at relatively low doses, such as 50 nM in vitro and 1 mg/kg body weight in vivo.

物理化学性质&存储条件

分子量	574.62
分子式	C30H38O11
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1S,2aR,3aS,3bS,4R,5aR,6R,7R,9S,9aS,9bR,11R,11aR,14R)-1-(Furan-3-yl)-4,9,14-trihydroxy-3b,6,11a-trimethyl-10-oxotetradecahydro-1H-6,9a-(methanooxymethano)naphtho[1',2':6,7]indeno[1,7a-b]oxirene-7,11-diyl diacetate

参考文献

1. Yang F, et al. Sci Transl Med. 2023 Feb 15;15(683):eabq3558.

Toosendanin

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Toosendanin

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