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化學性質:
規(guī)格 | 100mg 250mg 500mg |
CAS | 1332881-26-1 |
別名 | N/A |
化學名 | N/A |
分子式 | C21H19N3O4 |
分子量 | 377.39 |
溶解度 | Soluble in DMSO |
儲存條件 | 4°C, away from moisture and light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer[1][2][3]. tubulin[1]
VERU-111 (2.5-80 nM; 24-48 hours) inhibits Panc-1, AsPC-1 and HPAF-II cells growth in a dose and time-dependent manner (24 hours: IC50s of 25, 35 and 35 nM, respectively; 48 hours: IC50s of 11.8, 15.5, and 25 nM, respectively)[4].VERU-111 (5-20 nM; 24 hours) arrests Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner[4]. VERU-111 (5-20 nM; 24 hours) shows dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9, induces the expression of Bax and Bad, and inhibits the expression of Bcl-2 and Bcl-xl proteins in both AsPC-1 and Panc-1 cells[4]. Cell Proliferation Assay[4] Cell Line: Panc-1, AsPC-1, HPAF-II cells
VERU-111 (50 μg/mouse; intra-tumorally; 3 times per week for 3 weeks) effectively inhibits tumor growth as compared to vehicle-treated group. None of the mouse showed any apparent toxicity as constant increase of body weight in VERU-111 treated mice[4]. Animal Model: Six-week-old female athymic nude mice (bearing AsPC-1 cells)
[1]. Wang Q, et al. Structure-Guided Design, Synthesis, and Biological Evaluation of (2-(1H-Indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl) Methanone (ABI-231) Analogues Targeting the Colchicine Binding Site in Tubulin. J Med Chem. 2019 Jul 12. [2]. Qinghui Wang, et al. Discovery of ABI-231 analogs targeting the colchicine site in tubulin for advanced melanoma. Cancer Research 76(14 Supplement):4848-4848. [3]. Vivek Kashyap, et al. ABI-231: A novel small molecule suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting Human papilloma virus (HPV) E6 and E7. Cancer Research 78(13 Supplement):679-679. [4]. Kashyap VK, et al. Therapeutic efficacy of a novel βIII/βIV-tubulin inhibitor (VERU-111) in pancreatic cancer. J Exp Clin Cancer Res. 2019 Jan 23;38(1):29.
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原創(chuàng)作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業(yè)部
賬 號:2169 2341 6278