141172-08-9
141172-08-9 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)414.3±40.0 °C(Predicted)
密度1.089±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
常見問題列表
生物活性
SS28是具有口服生物利用度的SRT501 類似物,可抑制微管蛋白聚合,在G2/M引起細(xì)胞周期阻滯。SS28會(huì)引起細(xì)胞凋亡而不是壞死。靶點(diǎn)
Tubulin.
體外研究
SS28 (0-20 μM) induces cytotoxicity in different cancer cell lines.
SS28 treatment (5 μM for A549 and 2 μM for CEM) results in cell cycle arrest at G2/M phase leading to apoptosis upon further incubation.
Cell Proliferation Assay
Cell Line: | CEM, Reh, Nalm6, SUDHL8, Molt4, A549, HeLa 293T cells. |
Concentration: | 1, 5, 10 and 20 μM. |
Incubation Time: | 48 and 72 h. |
Result: | CEM and A549 exhibited maximum sensitivity to SS28 followed by SUDHL8, Molt4 and Reh, whereas Nalm6 showed moderate sensitivity after 48 h of the treatment. IC 50 values of SS28 in CEM and A549 cell line were 2.6 and 5.2 μM, respectively, whereas in SUDHL8, Molt4, Reh and Nalm6 were 2.7, 5.1, 7.9 and 21 μ M, respectively after 48 h of treatment. |
Cell Cycle Analysis
Cell Line: | CEM and A549 cells. |
Concentration: | 2 μM (CEM) and 5 μM (A549). |
Incubation Time: | 6, 12, 18, 24 and 30 h. |
Result: | Showed significant accumulation of cells at G2/M phase in a time-dependent manner (6 to 24 h) and a subsequent increase in the sub-G1 population, indicative of apoptosis at 30 h in case of A549. Similarly, studies in CEM also showed a distinct G2/M arrest after 12 h of treatment, as compared to vehicle control. |
體內(nèi)研究
SS28 (15 mg/kg. b.wt.) treatment results in inhibition of tumor cell proliferation.
Animal Model: | BALB/c mice using EAC cells. |
Dosage: | 15 mg/kg. |
Administration: | Orally on every alternate day for 9 doses. |
Result: | There was no further tumor progression in the mice when SS28 was administered, unlike the untreated tumor control mice. |