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化學(xué)性質(zhì):
規(guī)格 | 1mg 5mg 10mg |
CAS | 36707-00-3 |
別名 | N/A |
化學(xué)名 | 4-amino-5,8-dihydro-5-oxo-8-β-D-ribofuranosyl-pyrido[2,3-d]pyrimidine-6-carboxamide |
分子式 | C13H15N5O6 |
分子量 | 337.3 |
溶解度 | DMSO : 5.8 mg/mL (15.45 mM) |
儲存條件 | Store at -20°C |
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(chǎn)品描述:
API-1 is an inhibitor of Akt that reduces the level of phosphorylated Akt (IC50 = ~0.8 uM in OVCAR3 cells) by binding to Akt and blocking its translocation to the cell membrane. It reduces cell proliferation in various cancer cell lines, induces apoptosis, and, at a dose of 10 mg/kg per day, decreases tumor growth in a mouse xenograft model. API-1 inhibition of Akt leads to proteasomal degradation of the downstream mediator Mcl-1. Likely independent of Akt binding, API-1 inhibits cell growth (IC50s = 2-5 uM) and induces apoptosis in non-small cell lung and head and neck squamous cancer (NSCLC and HNSCC) cell lines with concomitant increases in caspase-3, -8, and -9 cleavage. It reduces the levels of cellular FLICE-inhibitory protein (c-FLIP), an important regulator of apoptosis, through ubiquitin- and proteasome-mediated degradation. It also has a synergistic effect on apoptosis in combination with TRAIL/APO-2L.The information regarding the reduction in phosphorylated Akt levels, IC50 value, translocation, cell proliferation, and xenograft tumor growth was drawn from a paper that has been retracted; however, the information specified in the retraction statement has not been included.
特別提醒:
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原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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開 戶 行:中國銀行山東省分行營業(yè)部
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