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编 号:F752156
分子式:C48H40N6O10
分子量:860.87
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生物活性:
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity.

体内研究:
IDO/Tubulin-IN-2 (HT2) (30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth.IDO/Tubulin-IN-2 (30 mg/kg; IV; 29 days) has effective antitumor immunity ability to promote the tumor therapeutic efficacy.Animal Model:ICR mice (mouse liver cancer xenograft models, established by subcutaneous inoculation of H22 cells)
Dosage:30 mg/kg
Administration:Intravenously injected via a tail vein; daily, for 21 days
Result:Significantly inhibited tumor growth.
Animal Model:Male A549 tumor xenograft BALB/c nude mice (5 weeks, 18-22 g)
Dosage:30 mg/kg
Administration:IV, daily, for 29 days
Result:Had effective antitumor immunity ability to promote the tumor therapeutic efficacy.

体外研究:
IDO/Tubulin-IN-2 (HT2) (0-50 μM, 4 h) shows potent cytotoxicity with IC50 values between 0.036 and 0.43 μM against cancer cell lines.IDO/Tubulin-IN-2 (0.1 μM, 24 h) arrests the HepG2 cells cycle mainly at the G2 phase.IDO/Tubulin-IN-2 (0.1 μM, 24 h) can effectively cause cell apoptosis.IDO/Tubulin-IN-2 (0.1 μM, 24 h) has strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3.IDO/Tubulin-IN-2 (0.05 μM, 24, 48 and 72 h) markedly decreases mRNA expression level of TDO at a time-dependent manner.IDO/Tubulin-IN-2 (2 days) can improve T-cell activation and proliferation and enhance immune response.
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