CAS NO: | 1255517-76-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | PF-4708671 is a potent cell-permeableS6K1inhibitor with aKiof 20 nM andIC50of 160 nM. | ||||||||||||||||
体外研究 (In Vitro) | PF-4708671 inhibits the activity of full-length S6K1 in vitro with a Kiof 20 nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with an IC50of 0.16 μM, and only inhibits very weakly the closely related S6K2 isoform (IC50of 65 μM). PF-4708671 inhibits RSK1 (IC50of 4.7 μM) and RSK2 (IC50of 9.2 μM) over 20-fold less potently than S6K1. PF4708671 inhibits MSK1 (IC50of 0.95 μM) 4-fold more weakly than S6K1[1]. HCT116 cells are treated with (i) vehicle (DMSO), (ii) OSI-906 (5 μM), (iii) PF-4708671 (10 μM), and (iv) OSI-906 (5 μM)+PF-4708671 (10 μM) for various amounts of time. HCT116 cells treated with OSI-906 alone (closed square) or PF4708671 alone (open circle) slightly inhibit cell growth. In contrast, proliferation in HCT116 cells is significantly inhibited after a 2-day treatment with the combination of OSI-906 and PF-4708671 (closed circle). A similar result is also observed when SW480 cells are treated with the combination of OSI-906 and PF-4708671. Colony formation also significantly reduces in OSI-906+PF-4708671-treated cells comparing with vehicle, OSI-906 alone, or PF-4708671 alone treated HCT116 or SW480 cells[2]. | ||||||||||||||||
体内研究 (In Vivo) | The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI-906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment[2]. | ||||||||||||||||
分子量 | 390.41 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H21F3N6 | ||||||||||||||||
CAS 号 | 1255517-76-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(85.37 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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