Tesetaxel  (Synonyms: DJ-927)

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].

Tesetaxel inhibits porcine brain tubulin depolymerization with an IC₅₀ of 0.44 μM and does not inhibit tubulin polymerization (IC₅₀ >2.0 μM)^[1].
Tesetaxel shows mean GI₅₀ value of 0.550 ng/mL against the 23 different human tumor cells^[1].
Tesetaxel exhibits greater cytotoxicity than Paclitaxel (HY-B0015) and Docetaxel (HY-B0011) against P-gp-overexpressing resistant PC-6 and HCT116 cell lines^[1].
Tesetaxel (10 days) inhibits colony formation of M5076 cells with an IC₅₀ of 5.5 ng/mL, and its activity is unaffected by the P-gp modulator Verapamil (HY-14275)^[1].

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

Tesetaxel (9.80 mg/kg; p.o.; q8d; 2 doses) achieves greater than 90% tumor growth inhibition against P-glycoprotein-positive human colon cancer DLD-1 xenografts in male BALB/c-nu/nu mice^[1].
Tesetaxel (12 mg/kg; p.o.; single dose) achieves greater than 90% tumor growth inhibition against P-glycoprotein-positive human breast cancer DU4475 xenografts in male BALB/c-nu/nu mice^[1].
Tesetaxel (9.8 mg/kg; p.o. or i.v.; once every 8 days; 2 doses) prolongs the life o in male C57BL/6 mice with P-glycoprotein-positive M5076 liver metastatic tumors^[1].

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

881.98

C₄₆H₆₀FN₃O₁₃

333754-36-2

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.