IDO/Tubulin-IN-2 (HT2) 是一种有效的TDO和微管蛋白 (tubulin)抑制剂。IDO/Tubulin-IN-2 对 U87、HepG2、A549、HCT-116 和 LO2 癌细胞具有较强的抗肿瘤活性，其IC50分别为 0.43、0.036、0.041、0.095和1.04 μM。IDO/Tubulin-IN-2 显著提高抗肿瘤活性。
| 生物活性 | IDO/Tubulin-IN-2 (HT2) is a potentTDOandtubulininhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2cancercell lines, withIC50values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity[1]. |
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体外研究
(In Vitro) | IDO/Tubulin-IN-2 (HT2) (0-50 μM, 4 h) shows potent cytotoxicity withIC50values between 0.036 and 0.43 μM against cancer cell lines[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) arrests the HepG2 cells cycle mainly at the G2 phase[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) can effectively cause cell apoptosis[1].
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[1].
IDO/Tubulin-IN-2 (0.05 μM, 24, 48 and 72 h) markedly decreases mRNA expression level of TDO at a time-dependent manner[1].
IDO/Tubulin-IN-2 (2 days) can improve T-cell activation and proliferation and enhance immune response[1].
Cell Proliferation Assay | Cell Line: | Human cancer cell lines and non-tumoral cell line[1] | | Concentration: | 0-50 μM | | Incubation Time: | 4 h | | Result: | Displayed potent cytotoxicity with IC50values of 0.43 μM (U87), 0.036 μM (HepG2), 0.041 μM (A549), 0.095 μM (HCT-116), and 1.04 μM (LO2). |
Cell Cycle Analysis | Cell Line: | HepG2 cells[1] | | Concentration: | 0.1 μM | | Incubation Time: | 24 h | | Result: | Arrested the HepG2 cells cycle mainly at the G2 phase. |
Apoptosis Analysis | Cell Line: | HepG2 cells[1] | | Concentration: | 0.1 μM | | Incubation Time: | 24 h | | Result: | Effectively caused cell apoptosis, the percentage of apoptosis cells increased to 54% |
Western Blot Analysis | Cell Line: | HepG2 cells[1] | | Concentration: | 0.1 μM | | Incubation Time: | 24 h | | Result: | Showed strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3, which could lead to cell death at last. |
RT-PCR | Cell Line: | HepG2 cells[1] | | Concentration: | 0.05 μM | | Incubation Time: | 24, 48 and 72 h | | Result: | Markedly decreased mRNA expression level of TDO at a time-dependent manner. |
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体内研究
(In Vivo) | IDO/Tubulin-IN-2 (HT2) (30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth[1].
IDO/Tubulin-IN-2 (30 mg/kg; IV; 29 days) has effective antitumor immunity ability to promote the tumor therapeutic efficacy[1].
| Animal Model: | ICR mice (mouse liver cancer xenograft models, established by subcutaneous inoculation of H22 cells)[1] | | 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)[1] | | Dosage: | 30 mg/kg | | Administration: | IV, daily, for 29 days | | Result: | Had effective antitumor immunity ability to promote the tumor therapeutic efficacy. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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