333754-36-2
Chemical Structure
Tesetaxel
Synonym(s): DJ-927
- CAS No.: 333754-36-2
- Formula:C46H60FN3O13
- Molecular Weight:881.98
IUPAC Name: (2aS,2bR,3S,4S,6S,8aR,10R,11aS,11bR,13aR)-2a-acetoxy-6-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-3-(3-fluoropyridin-2-yl)-2-hydroxypropanoyl)oxy)-10-((dimethylamino)methyl)-4-hydroxy-7,11b,14,14-tetramethyl-2a,2b,3,4,5,6,8a,11a,11b,12,13,13a-dodecahydro-2H-4,8-methanooxeto[3'',2'':3',4']benzo[1',2':3,4]cyclodeca[1,2-d][1,3]dioxol-3-yl benzoate
InChIKey: MODVSQKJJIBWPZ-VLLPJHQWSA-N
SMILES: CC(O[C@]12[C@]3([H])[C@]([C@@]4([H])[C@@](O[C@H](O4)CN(C)C)([H])C5=C(C)[C@@H](OC([C@H](O)[C@H](C6=C(C=CC=N6)F)NC(OC(C)(C)C)=O)=O)C[C@@](O)([C@H]3OC(C7=CC=CC=C7)=O)C5(C)C)(CC[C@@]1([H])OC2)C)=O
Biological Activity: Tesetaxel (DJ-927) is an orally active and brain-penetrant taxane tubulin inhibitor. Tesetaxel inhibits tubulin depolymerization with an IC50 of 0.44 μM. Tesetaxel inhibits cancer cells proliferation and shows potent antitumor activity against P-glycoprotein-positive cancer cells. Tesetaxel can be used for the research of cancer, such as solid tumors, liver metastasis, and advanced breast cancer[1][2].
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Tesetaxel | Tesetaxel (DJ-927) is an orally active and brain-penetrant taxane tubulin inhibitor. Tesetaxel inhibits tubulin depolymerization with an IC50 of 0.44 μM. Tesetaxel inhibits cancer cells proliferation and shows potent antitumor activity against P-glycoprotein-positive cancer cells. Tesetaxel can be used for the research of cancer, such as solid tumors, liver metastasis, and advanced breast cancer. | |||||||||||||||||||||
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- [1]. Shionoya M, et al. DJ-927, a novel oral taxane, overcomes P-glycoprotein-mediated multidrug resistance in vitro and in vivo. Cancer Sci. 2003;94(5):459-466. [Content Brief]
- [2]. James, Joyce, et al. "Tesetaxel, a novel, oral taxane, crosses intact blood-brain barrier (BBB) at therapeutically relevant concentrations." Cancer Research 79.13_Supplement (2019): 3078-3078.
Keywords
